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Moderate Activity (moderate + activity)
Selected AbstractsNickel(II) complexes bearing pyrazolylimine ligand: synthesis, structure, and catalytic properties for vinyl-type polymerization of norborneneAPPLIED ORGANOMETALLIC CHEMISTRY, Issue 4 2010Yuan-yuan Wang Abstract Two nickel(II) complexes of {2-[C3HN2(R1)2 -3,5]}[C(R2)N(C6H3iPr2 -2,6)]NiBr2 (complex 1: R1 = CH3, R2 = 2,4,6-trimethylphenyl; complex 2: R1 = R2 = Ph) were synthesized and characterized. The solid-state structure of complex 1 has been confirmed by X-ray single-crystal analysis. Activated by methylaluminoxane (MAO), complexes 1 and 2 are capable of catalyzing the polymerization of norbornene with moderate activities [up to 10.56 × 105 gPNBE (mol Ni h),1] with high molecular weights (Mw,13.56 × 105 g mol,1) and molecular weight distributions were around 2. The influences of polymerization parameters such as reaction temperature and Al,Ni molar ratio on catalytic activity and molecular weight of the polynorbornene were investigated in detail. The obtained polynorbornenes were characterized by means of 1H-NMR and FTIR techniques. The analytical results of polymer structures indicated that the norbornene polymerization is vinyl-type polymerization rather than ROMP. Copyright © 2009 John Wiley & Sons, Ltd. [source] Aqueous phase carbon dioxide and bicarbonate hydrogenation catalyzed by cyclopentadienyl ruthenium complexesAPPLIED ORGANOMETALLIC CHEMISTRY, Issue 11 2007Sylvain S. Bosquain Abstract The water-soluble ruthenium(II) complexes [Cp,RuX(PTA)2]Y and [CpRuCl(PPh3)(mPTA)]OTf (Cp, = Cp, Cp*, X = Cl and Y = nil; or X = MeCN and Y = PF6; PTA = 1,3,5-triaza-7-phosphaadamantane; mPTA = 1-methyl-1,3,5-triaza-7-phosphaadamantane) were used as catalyst precursors for the hydrogenation of CO2 and bicarbonate in aqueous solutions, in the absence of amines or other additives, under relatively mild conditions (100 bar H2, 30,80 °C), with moderate activities. Kinetic studies showed that the hydrogenation of HCO3, proceeds without an induction period, and that the rate strongly depends on the pH of the reaction medium. High-pressure multinuclear NMR spectroscopy revealed that the ruthenium(II) chloride precursors are quantitatively converted into the corresponding hydrides under H2 pressure. Copyright © 2007 John Wiley & Sons, Ltd. [source] Synthesis and Neurotrophic Activities of N-p -Tolyl/phenylsulfonyl L -Amino Acid Thiolester DerivativesCHINESE JOURNAL OF CHEMISTRY, Issue 3 2008Zhan-Nan YANG Abstract Various N-p- tolyl/phenylsulfonyl L -amino acid thiolester derivatives were designed and synthesized according to combination of functional groups. The synthesized compounds were identified by spectral methods (1H NMR, 13C NMR, MS and HRMS). Preliminary bioassays indicated that the compounds 4a, 4b, 4d, 5c, 5d, 5g, 6b and 6d showed remarkable activities and the compounds 4c, 5b and 6c showed moderate activities to inhibit anoxic damage of PC12 cells at 10 µg/mL, but the compounds 4d and 6d only showed moderate protective activities against PC12 cells at 5 µg/mL. Preliminary bioassays also indicated that the compounds 4c, 5a, 5c, 5d, 5e and 6b showed moderate activities to induce PC12-differentiation at 10 µg/mL. [source] Synthesis and Characterisation of (Alkoxybenzimidazolin-2-ylidene)palladium Complexes: The Effect of Ancillary Ligands on the Behaviour of PrecatalystsEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 13 2009Murray V. Baker Abstract A series of new N-heterocyclic carbene (NHC),palladium(II) complexes bearing electron-rich benzimidazolin-2-ylidene ligands are described and structurally and spectroscopically characterised. These (benzimidazolin-2-ylidene)palladium complexes bear butoxy groups to increase the solubility and perhaps influence the catalytic activity by increasing the electron density around the metal centre. The effect of varying the ancillary ligands is investigated, although these ligands do not appear to significantly alter the activity of the complexes as precatalysts. Preliminary studies indicate the complexes act as precatalysts with moderate activity in the Mizoroki,Heck and Suzuki,Miyaura coupling reactions. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009) [source] Composition and antifungal activity of essential oils isolated from Hypericum hyssopifolium and Hypericum heterophyllumFLAVOUR AND FRAGRANCE JOURNAL, Issue 1 2004A. Cakir Abstract The composition of the hydrodistilled essential oils obtained from the aerial parts of Hypericum hyssopifolium subsp. elongatum var. elongatum and H. heterophyllum Vent. were analysed by means of GC and GC,MS, and 66 compounds were determined in total. The oils showed remarkable differences in chemical composition. The oil of H. hyssopifolium, which is rich in monoterpenes, consists primarily of , -pinene (57.3%), , -pinene (9.0%), limonene (6.2%) and , -phellandrene (4.4%). The oil of H. heterophyllum was a complex mixture consisting mainly of sesquiterpenes (72.9% of the total oil). In this oil, isocaryophyllene (17.1%), , -pinene (11.6%), , -cadinene (9.5%), , -muurolene (8.2%), n -decane (5.8%), , -cadinene (5.5%) and , -caryophyllene (4.5%) were found to be major constituents. The two essential oils were tested for antifungal activity using microbial growth inhibition assays in vitro against 10 agricultural pathogenic fungi, which consisted of ,ve Fusarium species (F. oxysporum, F. culmorum, F. sambucinum, F. solani and F. acuminatum) and ,ve anastomosis groups of Rhizoctonia solani (AG-3, AG-4, AG-5, AG-9 and AG-11). In general, the oils showed moderate activity against several fungal species, viz F. acuminatum, AG-5 and AG-11. The most signi,cant results were obtained against AG-11 for H. heterophyllum oil. However, both oils increased the growth of some fungal species. In addition, the antifungal activity of 13 pure compounds identi,ed as major components in the essential oils of the Hypericum species studied were determined using microbial growth inhibition assays against the 10 fungal species mentioned above. Among these compounds, both , -caryophyllene oxide and , -terpineol were inhibitory to the growth of all fungi. Copyright © 2003 John Wiley & Sons, Ltd. [source] Phase II trial of taxol in salivary gland malignancies (E1394): A trial of the Eastern Cooperative Oncology GroupHEAD & NECK: JOURNAL FOR THE SCIENCES & SPECIALTIES OF THE HEAD AND NECK, Issue 3 2006Jill Gilbert MD Abstract Background. Malignant tumors of the salivary glands make up approximately 5% of head and neck cancers. The Eastern Cooperative Oncology Group (ECOG) initiated a phase II evaluation of paclitaxel in patients with locally recurrent or metastatic salivary gland malignancies. Methods. Chemo-naive patients with histologically confirmed recurrent or metastatic carcinoma of salivary gland origin (mucoepidermoid, adenocarcinoma, or adenoid cystic) were eligible. Patients were treated with paclitaxel, 200 mg/m2 IV, every 21 days for a minimum of four cycles. Results. Forty-five patients were treated. Eight partial responses were seen among the 31 patients with mucoepidermoid or adenocarcinoma histologic findings for a response rate of 26%. No responses were seen in the adenoid cystic carcinoma group. No significant difference in overall survival was found among these three histologic subgroups. Conclusion. Paclitaxel demonstrates moderate activity in salivary gland tumors of mucoepidermoid and adenocarcinoma histology. The poor response rate in adenoid cystic carcinoma is consistent with prior reports in this chemoresistant histologic subtype. © 2006 Wiley Periodicals, Inc. Head Neck28: 197,204, 2006 [source] New Diterpenoid Alkaloids from Aconitum recemulosumFranch.HELVETICA CHIMICA ACTA, Issue 9 2009Yong-Hui Ge Abstract Two new diterpenoid alkaloids, racemulosines A (1) and B (2), were isolated from the roots of Aconitum racemulosumFranch. The structures of the new alkaloids were elucidated by analysis of physical and spectroscopic data, and the structure of 1 was further confirmed by a single-crystal X-ray diffraction analysis. Furthermore, compound 1, at 2.25,10,4,mol/l, showed moderate activity against platelet aggregation induced by PAF (platelet-activation factor). [source] Active Crohn's disease and ulcerative colitis can be specifically diagnosed and monitored based on the biostructure of the fecal floraINFLAMMATORY BOWEL DISEASES, Issue 2 2008Alexander Swidsinski MD Abstract Background: The intestinal microflora is important in the pathogenesis of inflammatory bowel disease (IBD). The impact of its spatial organization on health and disease is unknown. Methods: We investigated sections of paraffin-embedded punched fecal cylinders. Fluctuations in spatial distribution of 11 bacterial groups were monitored in healthy subjects (n = 32), patients with IBD (n = 204), and other gastrointestinal diseases (n = 186) using fluorescence in situ hybridization (FISH). Results: The microbial structure differed in patients with Crohn's disease (CD), ulcerative colitis (UC), and healthy and disease controls. The profiles of CD and UC were distinctly opposite in 6 of 11 FISH probes used. Most prominent were a depletion of Faecalibacterium prausnitzii (Fprau<1 × 109/mL) with a normal leukocyte count in CD and a massive increase of leukocytes in the fecal-mucus transition zone (>30 leukocytes/104,m2) with high Fprau in patients with UC. These 2 features alone enabled the recognition of active CD (Crohn's Disease Activity Index [CDAI] >150) or UC (Clinical Activity Index [CAI] >3) with 79%/80% sensitivity and 98%/100% specificity. The mismatch in the sensitivity was mainly due to overlap between single IBD entities, and the specificity was exclusively due to the similarity of Crohn's and celiac disease. When inflammatory bowel disease (IBD) patients were pooled the sensitivity was 100% for severe disease, 84% for moderate activity, 72% for IBD with ,12 months remission, and 24% for IBD with >12 months remission. Conclusions: The fecal flora is highly structured and spatially organized. Diagnosing IBD and monitoring disease activity can be performed based on analysis of punched fecal cylinders independent from the patient's complaints. (Inflamm Bowel Dis 2007) [source] Can physical activity modulate pancreatic cancer risk? a systematic review and meta-analysisINTERNATIONAL JOURNAL OF CANCER, Issue 12 2010Michael A. O'Rorke Abstract Numerous epidemiological studies have examined the association between physical activity and pancreatic cancer; however, findings from individual cohorts have largely not corroborated a protective effect. Among other plausible mechanisms, physical activity may reduce abdominal fat depots inducing metabolic improvements in glucose tolerance and insulin sensitivity, thereby potentially attenuating pancreatic cancer risk. We performed a systematic review to examine associations between physical activity and pancreatic cancer. Six electronic databases were searched from their inception through July 2009, including MEDLINE and EMBASE, seeking observational studies examining any physical activity measure with pancreatic cancer incidence/mortality as an outcome. A random effects model was used to pool individual effect estimates evaluating highest vs. lowest categories of activity. Twenty-eight studies were included. Pooled estimates indicated a reduction in pancreatic cancer risk with higher levels of total (five prospective studies, RR: 0.72, 95% CI: 0.52,0.99) and occupational activity (four prospective studies, RR: 0.75, 95% CI: 0.59,0.96). Nonsignificant inverse associations were seen between risks and recreational and transport physical activity. When examining exercise intensity, moderate activity appeared more protective (RR: 0.79, 95% CI: 0.52,1.20) than vigorous activity (RR: 0.97, 95% CI: 0.85,1.11), but results were not statistically significant and the former activity variable incorporated marked heterogeneity. Despite indications of an inverse relationship with higher levels of work and total activity, there was little evidence of such associations with recreational and other activity exposures. [source] The dual EGFR/HER-2 tyrosine kinase inhibitor lapatinib sensitizes colon and gastric cancer cells to the irinotecan active metabolite SN-38INTERNATIONAL JOURNAL OF CANCER, Issue 12 2009Melissa J. LaBonte Abstract Members of the human epidermal receptor (HER) family are frequently associated with aggressive disease and poor prognosis in multiple malignancies. Lapatinib is a dual tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR) and HER-2. This study evaluated the therapeutic potential of lapatinib, alone and in combination with SN-38, the active metabolite of irinotecan (CPT-11), in colon and gastric cancer cell lines. Concentration-dependent antiproliferative effects of both lapatinib and SN-38 were observed in all colon and gastric cancer cell lines tested but varied significantly between individual cell lines (lapatinib range 0.08,11.7 ,M; SN-38 range 3.6,256 nM). Lapatinib potently inhibited the growth of a HER-2 overexpressing gastric cancer cell line and demonstrated moderate activity in gastric and colon cancer cells with detectable HER-2 expression. The combination of lapatinib and SN-38 interacted synergistically to inhibit cell proliferation in all colon and gastric cancer cell lines tested. Cotreatment with lapatinib and SN-38 also resulted in enhanced cell cycle arrest and the induction of apoptosis with subsequent cellular pharmacokinetic analysis demonstrating that lapatinib promoted the increased intracellular accumulation and retention of SN-38 when compared to SN-38 treatment alone. Finally, the combination of lapatinib and CPT-11 demonstrated synergistic antitumor efficacy in the LoVo colon cancer mouse xenograft model with no apparent increase in toxicity compared to CPT-11 monotherapy. These results provide compelling preclinical rationale indicating lapatinib to be a potentially efficacious chemotherapeutic combination partner for irinotecan in the treatment of gastrointestinal carcinomas. © 2009 UICC [source] Peptidase activity in various species of dairy thermophilic lactobacilliJOURNAL OF APPLIED MICROBIOLOGY, Issue 2 2004M. Gatti Abstract Aims:, The aim of the present work was to evaluate the enzymatic potential manifested by aminopeptidase activity of different thermophilic Lactobacillus biotypes and to measure the influence of cell growth phase on enzyme expression. Methods and Results:, The activities were evaluated by the hydrolysis of , -naphthylamide substrates for both whole and mechanically disrupted cells of L. helveticus, L. delbrueckii subsp. bulgaricus and L. delbrueckii subsp. lactis strains, collected from both the exponential and the stationary growth phase. In general, activities were higher for cells in the exponential rather than in the stationary phase and the disrupted cells showed higher activities than the whole cells. The highest activity expressed by all strains corresponded to X-prolyl-dipeptidyl aminopeptidase while a moderate activity was observed towards Arg- ,Na, Lys- ,Na and Leu- ,Na. The lowest activity was observed for Pro- ,Na. Conclusions:, It may be inferred that the cell structure and the cell physiology are crucial to define the level of efficiency of expression for aminopeptidase activity. The two species may be characterized by a different enzymatic system that hydrolyses N-terminal leucine. Significance and Impact of the Study:, The differences of peptidase activities in L. helveticus and L. delbrueckii species acquires an importance to comprehend their role in the biochemical events occurring in cheese ripening. [source] Habitual Levels of Physical Activity Influence Bone Mass in 11-Year-Old Children From the United Kingdom: Findings From a Large Population-Based Cohort,JOURNAL OF BONE AND MINERAL RESEARCH, Issue 1 2007Jon H Tobias MD Abstract We examined the influence of habitual levels of physical activity on bone mass in childhood by studying the relationship between accelerometer recordings and DXA parameters in 4457 11-year-old children. Physical activity was positively related to both BMD and bone size in fully adjusted models. However, further exploration revealed that this effect on bone size was modified by fat mass. Introduction: Exercise interventions have been reported to increase bone mass in children, but it is unclear whether levels of habitual physical activity also influence skeletal development. Materials and Methods: We used multivariable linear regression to analyze associations between amount of moderate and vigorous physical activity (MVPA), derived from accelerometer recordings for a minimum of 3 days, and parameters obtained from total body DXA scans in 4457 11-year-old boys and girls from the Avon Longitudinal Study of Parents and Children. The influence of different activity intensities was also studied by stratification based on lower and higher accelerometer cut-points for moderate (3600 counts/minute) and vigorous (6200 counts/minute) activity, respectively. Results: MVPA was positively associated with lower limb BMD and BMC adjusted for bone area (aBMC; p < 0.001, adjusted for age, sex, socio-economic factors, and height, with or without additional adjustment for lean and fat mass). MVPA was inversely related to lower limb bone area after adjusting for height and lean mass (p = 0.01), whereas a positive association was observed when fat mass was also adjusted for (p < 0.001). Lower limb BMC was positively related to MVPA after adjusting for height and lean and fat mass (p < 0.001), whereas little relationship was observed after adjusting for height and lean mass alone (p = 0.1). On multivariable regression analysis using the fully adjusted model, moderate activity exerted a stronger influence on lower limb BMC compared with light activity (light activity: 2.9 [1.2,4.7, p = 0.001]; moderate activity: 13.1 [10.6,15.5, p < 0.001]; regression coefficients with 95% confidence intervals and p values). Conclusions: Habitual levels of physical activity in 11-year-old children are related to bone size and BMD, with moderate activity exerting the strongest influence. The effect on bone size (as reflected by DXA-based measures of bone area) was modified by adjustment for fat mass, such that decreased fat mass, which is associated with higher levels of physical activity, acts to reduce bone size and thereby counteract the tendency for physical activity to increase bone mass. [source] Specificities of proteases for use in leather manufactureJOURNAL OF CHEMICAL TECHNOLOGY & BIOTECHNOLOGY, Issue 3 2006Farhad Foroughi Abstract Proteases are used in leather manufacture in the processes of soaking, unhairing and bating of hides and skins. However proteases can be relatively non-specific in their usage, and for improved efficacy of enzyme biocatalysis within the industry, an analysis of specific activities of enzymes towards skin proteins was undertaken. Most commercial proteases for soaking showed substantial activity against the substrates elastin,Congo Red and Azocoll but little or no activity against keratin,azure and hide powder black. Enzymes used for unhairing in conjunction with 30% of the usual concentration of sulfide to effect chemical unhairing showed moderate activity against all substrates tested (selected as representative of skin proteins), while proteases used in bating showed activity against Azocoll and elastin,Congo Red but had no keratinase activity and little activity against hide powder black. Bating proteases and soaking proteases displayed similar activities at pH 8. Microbes isolated in the screening of organisms from putrefied skins included one fungal and two bacterial isolates whose extracellular enzymes had efficient unhairing activity without the addition of sulfide. Enzyme activities for these proteases included high activity measured against Azocoll with little or no activity against elastin,Congo Red, keratin,azure and hide powder black. Neither elastase nor keratinase activities were determined as being essential for unhairing. Copyright © 2005 Society of Chemical Industry [source] Synthesis of trisubstituted thiophenes designed as progesterone receptor modulatorJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 5 2006Weiqin Jiang When a known 2-[4-morpholino]-3-aryl-5-substituted thiophene, which showed moderate activity as a progesterone antagonist, was superimposed with a potent steroidal progesterone antagonist Org-33628, it showed a fair alignment in most parts of the molecules. According to the molecular modelling, displacement of the morpholine oxygen atom in the thiophene derivative with a carbonyl group would provide a better alignment with the C-3 carbonyl in Org-33628. Thus, a series of novel trisubstituted thiophenes bearing a cyclic ketone moiety was synthesized. Although these compounds only showed weak activities as progesterone receptor antagonists, all target compounds are novel and are fully characterized. [source] Synthesis and antimicrobial activity of 2-substituted-2,3-dihydro-5-propoxy-1H -1,3,2-benzodiazaphosphole 2-OxidesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 1 2001M. Venugopal Several 2-alkylcarbamato/thiocarbamato/aryloxy/trichloromethyl-2,3-dihydro-5-propoxy-1H -1,3,2-benzodiazaphosphole 2-oxides (4 and 6) were synthesised by reacting 4-propoxy- o -phenylenediamine (1) with various N -dichlorophosphinyl carbamates (3), aryl phosphorodichloridates (5a-f) and trichloromethyl phosphonic dichloride (5g) in the presence of triethylamine at 45-65 °C. Their ir, 1H, 13C, 31P nmr and mass spectral data are discussed. The compounds were screened for antifungal activity against Curvularia lunata and Aspergillus niger and for antibacterial activity against Bacillus subtilis and Escherichia coli. Most of these compounds exhibited moderate activity in the assays. [source] Weight Management and Fruit and Vegetable Intake Among US High School Students*JOURNAL OF SCHOOL HEALTH, Issue 8 2008Richard Lowry MD ABSTRACT Background:, Consumption of fruits and vegetables is often recommended to promote healthy weight. The purpose of this study was to examine associations between fruit and vegetable intake and common weight management behaviors among US high school students who were trying to lose or stay the same weight. Methods:, Data from the 1999, 2001, and 2003 national high school Youth Risk Behavior Surveys were combined and the analyses stratified by gender (females, N = 16,709; males, N = 10,521). We considered 3 common weight management strategies,being physically active (ie, moderate activity for 30 minutes on 5 or more days per week or vigorous activity for 20 minutes on 3 or more days per week), eating a reduced calorie or fat diet, and limiting TV viewing. Sufficient fruit and vegetable intake was defined as eating 5 or more servings per day. Odds ratios (ORs) were calculated using logistic regression. Results:, Only 21.3% of females and 24.7% of males ate sufficient fruits and vegetables. Being physically active was associated with sufficient fruit and vegetable intake. Eating a reduced calorie or fat diet and limiting TV viewing (among males) were associated with sufficient fruit and vegetable intake only among physically active students. The odds of sufficient fruit and vegetable intake were greatest among female (OR = 3.01) and male (OR = 2.91) students who combined all 3 strategies (31.5% of females, 21.6% of males). Conclusions:, Interventions that promote fruit and vegetable intake within the context of healthy weight management may be more effective if they combine nutrition and physical activity strategies. Further research is needed to test this approach. [source] In vitro and in vivo pharmacodynamic properties of the fluoroquinolone ibafloxacinJOURNAL OF VETERINARY PHARMACOLOGY & THERAPEUTICS, Issue 6 2002M. Coulet The pharmacodynamic properties of a new veterinary fluoroquinolone antimicrobial agent, ibafloxacin, were evaluated. Minimal inhibitory concentrations (MIC), time-kill kinetics, postantibiotic effect (PAE) and postantibiotic subminimal inhibitory concentration effects (PA-SME) were determined against pathogenic canine Gram-negative and Gram-positive bacterial isolates from dermal, respiratory and urinary tract infections. The synergistic interactions between ibafloxacin and its main metabolite, 8-hydroxy-ibafloxacin were investigated. Finally, the efficacy of ibafloxacin was tested in in vivo canine infection models. Ibafloxacin had good activity against Pasteurella spp., Escherichia coli, Klebsiella spp., Proteus spp. and Staphylococcus spp. (MIC90=0.5 µg/mL), moderate activity against Bordetella bronchiseptica, Enterobacter spp. and Enterococcus spp. (MIC50=4 µg/mL) and low activity against Pseudomonas spp. and Streptococcus spp. The time-killing analysis confirmed that ibafloxacin was bactericidal with a broad spectrum of activity. The PAE and PA-SME were between 0.7,2.13 and 1,11.5 h, respectively. Finally, studies in dog models of wound infection and cystitis confirmed the efficacy of once daily oral ibafloxacin at a dosage of 15 mg/kg. Additional studies are needed to better define the importance of AUC/MIC (AUIC) and Cmax/MIC ratios on the outcome of fluoroquinolone therapy in dogs. [source] Inhibitors of biotin biosynthesis as potential herbicides: Part 2,PEST MANAGEMENT SCIENCE (FORMERLY: PESTICIDE SCIENCE), Issue 10 2005Tali Ashkenazi Abstract Isosteres and analogues of 7-keto-8-aminopelargonic acid (KAPA) and 7,8-diaminopelargonic acid (DAPA), the vitamer intermediates involved in the biosynthetic pathway of biotin, possessing chain lengths of eight carbon atoms, were prepared and evaluated as potential herbicides. The most active compounds, 7-amino-octanoic acid hydrochloride and 7-allyloxy-6-oxo-octanoic acid, displayed Arabidopsis GR50 (concentration of the active compound that causes a 50% growth inhibition) values of 5 and 10 mg kg,1 respectively. The DAPA analog 6,7-diamino-octanoic acid dihydrochloride, when tested in the greenhouse against six weed species, displayed moderate activity against three species, being most active against foxtail millet. Copyright © 2005 Society of Chemical Industry [source] Herbicidal action of 2-hydroxy-3-alkyl-1,4-naphthoquinonesPEST MANAGEMENT SCIENCE (FORMERLY: PESTICIDE SCIENCE), Issue 3 2002Philip J Jewess Abstract The main mode of herbicidal activity of 2-hydroxy-3-alkyl-1,4-naphthoquinones is shown to be inhibition of photosystem II (PSII). The herbicidal and in vitro activities have been measured and correlated with their (Log)octanol/water partition coefficients (Log Ko/w). The length of the 3- n -alkyl substituent for optimal activity differed between herbicidal and in vitro activity. The maximum in vitro activity was given by the nonyl to dodecyl homologues (Log Ko/w between 6.54 and 8.12), whereas herbicidal activity peaked with the n -hexyl compound (Log Ko/w,=,4.95). The effect of chain branching was also investigated using isomeric pentyl analogues substituted at position 3. All exhibited similar levels of in vitro activities but herbicidal activities differed, albeit moderately, with the exception of one analogue that was much less phytotoxic. Other modes of action were also investigated using two representative compounds. They did not show any activity on photosystem I or mitochondrial complex I, or generate toxic oxygen radicals by redox cycling reactions. Only moderate activity was found against mitochondrial complex III from plants, in contrast to much higher corresponding activity using an insect enzyme. © 2002 Society of Chemical Industry [source] Antifungal activity of Heterothalamus alienus metabolitesPHYTOTHERAPY RESEARCH, Issue 4 2008Adriana del V. Pacciaroni Abstract The chemical study of Heterothalamus alienus gave rutin, spathulenol (1), (1R,7S)-germacra-4(15),5,10(14)-trien-1, -ol (2), sakuranetin (3), padmatin 3-acetate (4), (2R,3R)-dihydroquercetin-7,3,,4,-trimethyl ether (5), (2R,3R)-dihydroquercetin-7,4,-dimethyl ether (6), (2R,3R)-3-acetoxy-5,7,4,-trihydroxyflavanone (7), as the main components of an antifungal extract of the aerial parts of the plant. Compound 2 showed moderate activity, with Epidermophyton floccosum being the most susceptible species (MIC = 100 µg/mL); compound 3 showed the best antifungal behavior having a broad spectrum of action and the lowest MICs. This flavanone along with flavanolol 5 showed very good activity against standardized (MIC = 31.2 µg/mL) as well as clinical isolates of Trichophyton rubrum and T. mentagrophytes (MIC ranges 31.2,62.5 µg/mL and 31.2,125 µg/mL, respectively) and demonstrated not only fungistatic but also fungicide properties. Flavanolol 6 was active against all the dermatophytes tested with MICs of 62.5,250 µg/mL. Rutin, spathulenol (1) and the 3-acetylated flavanones 4 and 7 were inactive or marginally active against the fungal panel. Copyright © 2008 John Wiley & Sons, Ltd. [source] Synthesis and Antiproliferative Activitiy of Novel Diaryl Ureas Possessing a 4H- Pyrido[1,2- a]pyrimidin-4-one GroupARCHIV DER PHARMAZIE, Issue 1 2010Peng Yao Abstract We herein disclose a series of novel diaryl urea derivatives possessing a 4H- pyrido[1,2 -a]pyrimidin-4-one group as novel potent anticancer compounds. The structures were confirmed by IR, 1H-NMR, and MS. All the compounds were screened for their antiprofilerative activity agaist the human breast cancer cell line (MDA-MB-231). The pharmacological results indicated that most of the compounds showed moderate activity. The best of this series is compound 4c (IC50 = 0.7 ,mol/L), with a potency 3.6-fold higher than Sorafenib (IC50 = 2.5 ,mol/L), which was approved in 2005. [source] Synthesis and Anti-HIV-1 Activity of 1-Substiuted 6-(3-Cyanobenzoyl) and [(3-Cyanophenyl)fluoromethyl]-5-ethyl-uracilsARCHIV DER PHARMAZIE, Issue 9 2009Yasser M. Loksha Abstract 1-Substiuted 6-(3-cyanobenzoyl) and [(3-cyanophenyl)fluoromethyl]-5-ethyl-uracils were synthesized and evaluated in cell-based assays against HIV-1 wild-type and its clinically relevant non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant mutants. Some of the synthesized compounds showed activity against HIV-1 wild-type in the same range as Emivirine (MKC-442). 3-{[3-(Allyloxymethyl)-5-ethyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl]fluoromethyl}-benzonitrile 11b showed moderate activity against the Y181C HIV-1 mutant strain. [source] Synthesis, Cytotoxicity and Antileishmanial Activity of Some N -(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-aminesCHEMICAL BIOLOGY & DRUG DESIGN, Issue 6 2010Elaine S. Coimbra We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3). Hydrolysis of the methyl ester adduct (5) yielded the free acid (6). The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells. [source] Joziknipholones A and B: The First Dimeric Phenylanthraquinones, from the Roots of Bulbine frutescensCHEMISTRY - A EUROPEAN JOURNAL, Issue 5 2008Gerhard Bringmann Prof. Abstract From the roots of the African plant Bulbine frutescens (Asphodelaceae), two unprecedented novel dimeric phenylanthraquinones, named joziknipholones A and B, possessing axial and centrochirality, were isolated, together with six known compounds. Structural elucidation of the new metabolites was achieved by spectroscopic and chiroptical methods, by reductive cleavage of the central bond between the monomeric phenylanthraquinone and -anthrone portions with sodium dithionite, and by quantum chemical CD calculations. Based on the recently revised absolute axial configuration of the parent phenylanthraquinones, knipholone and knipholone anthrone, the new dimers were attributed to possess the P -configuration (i.e., with the acetyl portions below the anthraquinone plane) at both axes in the case of joziknipholone A, whereas in joziknipholone B, the knipholone part was found to be M -configured. Joziknipholones A and B are active against the chloroquine resistant strain K1 of the malaria pathogen, Plasmodium falciparum, and show moderate activity against murine leukemic lymphoma L5178y cells. [source] Novel Metathesis Catalysts Based on Ruthenium 1,3-Dimesityl-3,4,5,6-tetrahydropyrimidin-2-ylidenes: Synthesis, Structure, Immobilization, and Catalytic ActivityCHEMISTRY - A EUROPEAN JOURNAL, Issue 22 2004Liangru Yang Dr. Abstract The synthesis of novel ruthenium-based metathesis catalysts containing the saturated 1,3-bis(2,4,6-trimethylphenyl)-3,4,5,6-tetrahydropyrimidin-2-ylidene ligand, that is, [RuCl2(NHC){CH-2-(2-PrO)-5-NO2 -C6H3}] (1) and [Ru(CF3COO)2(NHC){CH-2-(2-PrO)-5-NO2 -C6H3}] (2) (NHC=1,3-bis(2,4,6-trimethylphenyl)-3,4,5,6-tetrahydropyrimidin-2-ylidene) is described. Both catalysts are highly active in ring-closing metathesis (RCM) and ring-opening cross-metathesis (ROCM). Compound 1 shows moderate activity in enyne metathesis. Compound 2 is not applicable to enyne metathesis since it shows high activity in the cyclopolymerization of diethyl dipropargylmalonate (DEDPM). Poly(DEDPM) prepared by the action of 2 consists of 95,% five-membered rings, that is, poly(cyclopent-1-enevinylene)s, and 5,% of six-membered rings, that is, poly(cyclohex-1-ene-3-methylidene)s. The polymerization proceeds in a nonliving manner and results in polyenes with broad polydispersities (1.9,PDI,2.3). Supported analogues of 2 were prepared by immobilization on hydroxymethyl-Merrifield resin and a monolithic support derived from ring-opening-metathesis polymerization (ROMP). Catalyst loadings of 1 and 2.5,%, respectively, were obtained. Both supported versions of 2 showed excellent reactivity. With 0.24,2,% of the supported catalysts, yields in RCM and ROCM were in the range of 76,100,%. Leaching of ruthenium was low and resulted in Ru contaminations of the products of less than 0.000014,% (0.14 ppm). [source] [4-(2H -1,2,3-Benzotriazol-2-yl)phenoxy]alkanoic Acids as Agonists of Peroxisome Proliferator-Activated Receptors (PPARs)CHEMISTRY & BIODIVERSITY, Issue 4 2006Anna Sparatore Abstract A series of [4-(2H -1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids has been synthesized and tested as agonists of Peroxisome Proliferator-Activated Receptor (PPAR) ,, ,, and ,. Three compounds displayed 56 to 96% of maximal activity of the reference drug Wy-14643 on PPAR,, and two of these, i.e., 1 and 5, exhibited also moderate activity on either PPAR, or , with efficacy equal to 50% and 46% of that of rosiglitazone and GW 501516, respectively. Thus, compounds 1 and 5 represent interesting starting point for preparing novel agents for the treatment of dyslipidemia or of dyslipidemic type-2 diabetes. [source] Participation in organized weekly physical exercise in obese adolescents reduced daily physical activityACTA PAEDIATRICA, Issue 2 2009Maria Hagströmer Abstract Aim: The aim of this study was to describe the impact of organized weekly exercise for 13 weeks on aerobic fitness, objectively assessed habitual physical activity and body weight in obese adolescents. Methods: After inclusion and diagnostic evaluation, the adolescents were randomized to either an exercise group or to a control group which lasted for 13 weeks and consisted of a variety of group exercise activities. Out of 47 adolescents 31 (66%) could be evaluated, 16 in the exercise group and 15 in the control group. Results: After the intervention, the exercise group had decreased the daily time spent in moderate activity by 17 (32) min/day (p < 0.05), and the average intensity by 60 (96) counts/min (p < 0.05). A tendency for increased time spent in inactivity was found (37 min/day). No differences were seen in the control group for any of the variables measured. Conclusion: The exercise group showed, in contrast to expectations, a reduction in total daily physical activity with organized physical exercise compared to the control group. This may partly explain the failure of many intervention trials. [source] | ||||||||||||||||||||||||||||