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Phenyl
Kinds of Phenyl Terms modified by Phenyl Selected AbstractsSynthesis and structural conformation of N-substituted 1,4-dihyropyridine derivativesCRYSTAL RESEARCH AND TECHNOLOGY, Issue 1 2006M. Mahendra Abstract N-(Phenyl)-3,5-dicarbethoxy-2,6-dimethyl-4-(phenyl)-1,4-dihydropyridine (A) and N-(4-methoxy phenyl)--3,5 dicarbethoxy-2,6 dimethyl-4-(3-nitro phenyl)-1,4-dihydropyridine (B) has been synthesized as per scheme and characterized by the X-ray diffraction method. The compound A crystallizes in monoclinic space group P21/c with cell parameters a = 9.2770(11)Å, b = 8.6410(5)Å, c = 27.601(3)Å, , = 97.724(3)°, Z = 4. The compound B crystallizes in monoclinic space group P21/c with cell parameters a = 11.229(6), b = 12.746(7)Å, c =17.606(6)Å, , = 104.531(3)°, Z = 4. The structures exhibit both intra and intermolecular hydrogen bonds. Dihydropyridine ring of both the compounds adopt a flat boat conformation. (© 2005 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim) [source] Tripodands with Phenyl and Thiophenyl Rings and Nitrogen Bridgehead Atoms,EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 23 2006Martin Baier Abstract The flexible tripodands 7,9 and 15 with phenyl and thiophenyl rings as "legs" and nitrogen as bridgehead atoms have been synthesized by three-component condensation reactions of the corresponding amine with the aryl halide. The more rigid species 10,14 and 17 were built up from the podands 7,9 as well as from their iodine substitution products 33,35 by a sequence of ethynylation and C,C coupling reactions. Podand 16 was prepared from tris-iodide 36 by Sonogashira coupling with phenylacetylene. In the cases of 7, 12, 15,17, 22, 24, 35, 36, and 41 the structural parameters were determined by X-ray studies. With the exception of 7, 12, and 17, all structures show either close intermolecular contacts between heteroatoms (15, 22, 24, 35, and 36), C,H···N hydrogen bonding (41), or are closely packed as a result of ,···, stacking (16). We were able to isolate silver triflate complexes of 9, 10, and 16, and in the case of 9 we obtained crystals suitable for X-ray diffraction studies. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2006) [source] Stereoselective Synthesis of C- and N-Ketosides by Lewis Acid-Catalyzed C- and N-Glycosidation of Alkynyl, Phenyl, and Methyl KetosesEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 24 2003Ana M. Gómez Abstract C-Ketosides can be prepared conveniently, in a stereoselective manner, from alkynyl, phenyl and methyl glucopyranose hemiketals by reaction with carbon nucleophiles in the presence of Lewis acids. The reaction of the hemiketals with trimethylsilyl azide provides an efficient route to the corresponding N-ketopyranosides. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003) [source] Human salivary aggregation in Streptococcus intermedius type g strains: relationship with IgAFEMS IMMUNOLOGY & MEDICAL MICROBIOLOGY, Issue 2 2004Taihei Yamaguchi Abstract Bacterial aggregation is an important step in elimination from the human body to protect against infection. Streptococcus intermedius K1K aggregates in human saliva. In this study, the salivary agglutinin was identified. The aggregation level was very strong in sonic-treated saliva and 1-,m filtrate. Preincubation of human saliva with anti-human , chain serum or anti-human whole saliva serum completely inhibited aggregation, but preincubation with anti-human , chain serum or anti-Fc fragment of human IgG serum had no effect. Agglutinin of human saliva that could aggregate the strain K1K was purified using DEAE,Sepharose CL-6B, Phenyl,Sepharose CL-4B and Sephacryl S200HR gel filtration. Purified salivary agglutinin was characterized with electrophoresis and immunological techniques, indicating that purified material was IgA. Bacterial aggregation was dependent on the presence of calcium. Saliva filtrate specimens from eight healthy men and eight women showed different aggregation activities. Three men and one woman had little activity. These data show that the present bacterial aggregation was an immunoreaction between IgA in saliva and the bacteria dependent on the levels of calcium. In addition, the IgA in human saliva related with possible calcium-dependent antigen(s) on the surface of strain K1K. [source] Pharmacological interventions in aging and age-associated disordersGERIATRICS & GERONTOLOGY INTERNATIONAL, Issue 2 2007Kenichi Kitani In the present study, past attempts using different pharmaceuticals and chemicals which were reported to prolong lifespans of animals are critically reviewed. Despite a large number of trials in animals and humans, the validity of supplementation of antioxidant vitamins such as vitamins A, E and C for improving human health remains unresolved at present. A recent approach using antioxidant mimetics called the EUK series which, despite an initial enthusiastically reported success in prolonging the lifespan of nematodes, remains again unsettled because of the failure in reproducing the initial success by follow-up studies. ,-Phenyl- tert -butylnitrone and related nitrones were initially introduced as radical scavengers. Some of these (e.g. disodium 2,4-disulfophenyl-N- tert -butylnitrone) are at phase 3 clinical trials as an agent to treat cerebral stroke. This effect, however, appears at least in part to be related to signal transduction which makes these agents effective against cerebral stroke even when they are administered later than its onset. (,)Deprenyl is a monoamine oxidase-B inhibitor and has some neuroprotective and anti-apoptotic effects. The drug has also been shown to prolong the lifespans of at least four different animal species. The drug upregulates superoxide dismutase and catalase activities in selective brain regions of dopaminergic nature. These effects on antioxidant enzyme activities are suspected to be causally related to its effect on lifespans of animals. Future trials using these and other drugs are expected to open new doors for interventions in aging and age-associated disorders in humans. [source] Phenyl and Phenylethyl Glycosides from Picrorhiza scrophulariifloraHELVETICA CHIMICA ACTA, Issue 3 2004Sheng-Xiong Huang Three new phenyl glycosides, scrophenoside A (1), B (2), and C (3), and two new phenylethyl glycosides, scroside D (4) and scroside E (5), were isolated from the stem of Picrorhiza scrophulariifloraPennell (Scrophularlaceae), besides five known compounds. On the basis of spectroscopic evidence, the structures of the new compounds were elucidated as 4-acetyl-2-methoxyphenyl 6- O -[4-(, - D -glucopyranosyloxy)vanilloyl]- , - D -glucopyranoside (1), 4-acetylphenyl 6- O -[(E)- p -coumaroyl]- , - D -glucopyranoside (2), 4-[(1R)- and (1S)-1-hydroxyethyl]-2-methoxyphenyl , - D -glucopyranoside (3a and 3b, resp.), 2-(3,4-dihydroxyphenyl)ethyl O - , - D -glucopyranosyl-(1,3)-4- O -[(E)-feruloyl]- , - D -glucopyranoside (4), and 2-(3,4-dihydroxyphenyl)ethyl O - , - D -glucopyranosyl-(1,3)-6- O -[(E)-feruloyl]- , - D -glucopyranoside (5). [source] Synthesis of well-defined poly(p -benzamide) from chain-growth polycondensation and its application to block copolymersMACROMOLECULAR SYMPOSIA, Issue 1 2003Tsutomu Yokozawa Abstract Poly(p -benzamide) with a defined molecular weight and a low polydispersity and block copolymers containing this well-defined aramide was synthesized. Phenyl 4-(4-octyloxybenzylamino)benzoate (1b) polymerized at room temperature in the presence of base and phenyl 4-nitrobenzoate (2a) as an initiator in a chain-growth polycondensation manner to give well-defined aromatic polyamides having the 4-octyloxybenzyl groups as a protecting group on nitrogen in an amide. It was confirmed by a model reaction that deprotection of this protecting group proceeded completely with trifluoroacetic acid (TFA) without breaking the amide linkage. The utility of this approach to poly(p -benzamide) with a low polydispersity was demonstrated by the synthesis of block copolymers of poly(p -benzamide) and poly(N -octyl- p -benzamide) or poly(ethylene glycol). The SEM images of the supramolecular assemblies of the former block copolymer showed ,m-sized bundles and aggregates of flake structures. [source] Controlled Stability of Molecular Junctions,ANGEWANDTE CHEMIE, Issue 44 2009Diana Duli Der Einfluss der Grenzflächen auf Moleküldrähte mit Thiol-Endgruppen, die aus drei Phenyl- (P3) oder drei Thiophenringen (T3) bestehen, wurde mit der Bruchkontakt-Methode analysiert. Dabei wird die Leitfähigkeit G eines molekularen Kontakts gemessen (siehe REM-Bild des Kontakts und Schema der Molekülanordnung). Anders als beim T3-Molekül variiert G beim P3-Molekül stochastisch (siehe Diagramm). [source] N -Phenyl- N,-pyridylureas: stereochemical basis for anticonvulsant activityACTA CRYSTALLOGRAPHICA SECTION C, Issue 4 2006Arthur Camerman 4-[N -(2-Chloro-6-methylphenyl)ureido]pyridinium chloride, C13H13ClN3O+·Cl, (CI-953 hydrochloride), crystallizes with Z, = 2 in P. In both molecules, the methyl groups and Cl atoms on the benzene rings are disordered. The benzene rings of molecules A and B adopt two conformations, differing by a rotation of 180° about the C,N bond to the ureido group, in an approximate 1:1 ratio. This disorder is further enhanced by the rotation of the methyl groups in both adopted positions. The pyridine and benzene rings intersect at angles of 102.1,(1) and 111.3,(1)° for A and B, respectively. Hydrogen bonding is mediated by Cl, anions, resulting in indirect connectivity between the molecules. Superposition of the molecular structure, after 180° rotation about an amide bond, with that of phenytoin shows that the chemically different molecules possess stereochemical features in common, which may explain their common activities. [source] Synthesis and Antibacterial Activity of a New Series of 3-[3-(Substituted Phenyl)-1-Isonicotinoyl-1H -Pyrazol-5-yl]-2H -Chromen-2-one DerivativesARCHIV DER PHARMAZIE, Issue 6 2009Prashant Aragade Abstract A novel series of 3-[3-(substituted phenyl)-1-isonicotinoyl-1H -pyrazol-5-yl]-2H -chromen-2-one derivatives 4a,k have been synthesized by the reaction of 3-[2,3-dibromo-3-(substituted phenyl) propanoyl]-2H -chromen-2-one 3a,k and isonicotinic acid hydrazide in the presence of triethylamine in absolute ethanol, characterized by spectral data and screened for their in-vitro antibacterial activity against Gram-positive and Gram-negative bacteria. Among the series, compounds 4e, 4i, and 4k displayed an encouraging antibacterial activity profile as compared to the reference drug ampicillin against tested bacterial strains. [source] ChemInform Abstract: Cyclocondensation of N-Prop-2-ynyl- and N-Pentadiynyl-o-phenylenediamines with Phenyl Isothiocyanate.CHEMINFORM, Issue 21 2009R. V. Novikov Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Reaction of (2-Ethyl-aziridin-2-yl)diphenyl Methanol and Diphenyl-(2-phenyl-aziridin-2-yl)methanol with Phenyl and t-Butyl Isocyanates, Phenyl Isothiocyanate and Thiophosgene.CHEMINFORM, Issue 15 2008B. Kryczka Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: O-Arylation of Carboxylic Acids Using (Phenyl)[2-(trimethylsilyl)phenyl]iodonium Triflate as a Precursor of Arynes.CHEMINFORM, Issue 1 2008Jian Xue Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Gold-Catalyzed Intramolecular Carbothiolation of Alkynes: Synthesis of 2,3-Disubstituted Benzothiophenes (II) from (,-Alkoxy Alkyl) (ortho-Alkynyl Phenyl) Sulfides.CHEMINFORM, Issue 43 2006Itaru Nakamura Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Reaction of Cross-Conjugated Dienones with Phenyl- and 2-Pyridylhydrazines.CHEMINFORM, Issue 36 2006N. V. Sviridenkova Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis and Fungicidal Activities of 2-Silatranyl Propylamino-4-substituted Phenyl(hydrogen)-5,5-dimethyl-1,3,2-dioxaphosphinanes-2-oxides (Sulfides).CHEMINFORM, Issue 17 2006Shi-Guan Wan Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Enhancement in Antimicrobial Activity of 2-(Phenyl)-3-(2-butyl-4-chloro-1H-imidazolyl)-5-butylate Isoxazolidine.CHEMINFORM, Issue 30 2005M. P. Sadashiva Abstract For Abstract see ChemInform Abstract in Full Text. [source] Microwave Assisted Synthesis of Phenyl(2-phenyl-5,6,7,8-tetrahydro-4-quinolinyl)methanone and Its Derivatives.CHEMINFORM, Issue 11 2005H. Surya Prakash Rao Abstract For Abstract see ChemInform Abstract in Full Text. [source] Enantioselective Addition of Phenyl and Alkyl Acetylenes to Imines Catalyzed by Chiral Cu(I) Complexes.CHEMINFORM, Issue 9 2005Maurizio Benaglia Abstract For Abstract see ChemInform Abstract in Full Text. [source] Cobalt-Catalyzed Allylic Substitution Reaction of Allylic Ethers with Phenyl and Trimethylsilylmethyl Grignard Reagents.CHEMINFORM, Issue 49 2004Keiya Mizutani No abstract is available for this article. [source] Synthesis of Phenyl and Substituted Phenyl 3-Ethyl-2,3,5,9b-tetrahydro[1,3]oxazolo[2,3-a]isoindol-5-ones.CHEMINFORM, Issue 25 2004Dinesh S. Nair No abstract is available for this article. [source] ChemInform Abstract: Synthesis of Xanthenes, Indanes, and Tetrahydronaphthalenes via Intramolecular Phenyl,Carbonyl Coupling Reactions.CHEMINFORM, Issue 36 2001Chih-Wei Kuo Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Hydrolytic Reactions of Thymidine 5,- O -Phenyl- N -Alkylphosphoramidates, Models of Nucleoside 5,-Monophosphate ProdrugsCHEMISTRY - A EUROPEAN JOURNAL, Issue 30 2007Mikko Ora Dr. Abstract To obtain detailed data on the kinetics of hydrolytic reactions of triester-like nucleoside 5,- O -aryl- N -alkylphosphoramidates, potential prodrugs of antiviral nucleoside monophosphates, the hydrolysis of diastereomeric (RP/SP) thymidine 5,-{O -phenyl- N -[(1S)-2-oxo-2-methoxy-1-methylethyl]phosphoramidate} (3), a phosphoramidate derived from the methyl ester of L -alanine, has been followed by reversed-phase HPLC over the range from H0=0 to pH,8 at 90,°C. According to the time-dependent product distributions, the hydrolysis of 3 proceeds at pH<4 by two parallel routes, namely by nucleophilic displacement of the alaninyl ester moiety by a water molecule and by hydrolysis of the carboxylic ester linkage that allows intramolecular attack of the carboxy group on the phosphorus atom, thereby resulting in the departure of either thymidine or phenol without marked accumulation of any intermediates. Both routes represent about half of the overall disappearance of 3. The departure of phenol eventually leads to the formation of thymidine 5,-phosphate. At pH>5, the predominant reaction is hydrolysis of the carboxylic ester linkage followed by intramolecular displacement of a phenoxide ion by the carboxylate ion and hydrolysis of the resulting cyclic mixed anhydride into an acyclic diester-like thymidine 5,-phosphoramidate. The latter product accumulated quantitatively without any indication of further decomposition. Hydroxide-ion-catalyzed POPh bond cleavage of the starting material 3 occurred as a side reaction. Comparative measurements with thymidine 5,-{N -[(1S)-2-oxo-2-methoxy-1-methylethyl]phosphoramidate} (4) revealed that, under acidic conditions, this diester-like compound is hydrolyzed by PN bond cleavage three orders of magnitude more rapidly than the triester-like 3. At pH>5, the stability order is reversed, with 3 being hydrolyzed six times as rapidly as 4. Mechanisms of the partial reactions are discussed. [source] A New Amphiphilic Derivative, N -{[4-(Lactobionamido)methyl]benzylidene}- 1,1-dimethyl-2-(octylsulfanyl)ethylamine N -Oxide, Has a Protective Effect Against Copper-Induced Fulminant Hepatitis in Long,Evans Cinnamon Rats at an Extremely Low Concentration Compared with Its Original Form , -Phenyl- N -(tert -butyl) NitroneCHEMISTRY & BIODIVERSITY, Issue 9 2007Taketoshi Asanuma Abstract An amphiphilic , -phenyl- N- (tert -butyl) nitrone (PBN) derivative, N -{[4-(lactobionamido)methyl]benzylidene}-1,1-dimethyl-2-(octylsulfanyl)ethylamine N -oxide (LPBNSH), newly synthesized from its original form PBN in hopes of clinical use, was intraperitoneally administered to Long,Evans Cinnamon (LEC) rats every 2 days at the concentrations of 0.1, 0.5, 1.0, and 2.0,mg/kg. We found that LPBNSH protected against copper-induced hepatitis with jaundice in LEC rats at concentrations of 0.1 and 0.5,mg/kg, which were extremely low compared with that of PBN. It also effectively prevented the loss of body weight, reduced the death rate, and suppressed the increase in serum aspartate aminotransferase and alanine aminotransferase values arising from fulminant hepatitis with jaundice at the same concentrations. Similar results were observed when PBN was administered at the concentration of 150,mg/kg. Immunohistochemical analysis of 8-hydroxy-2,-deoxyguanosine and measurement of thiobarbituric acid-reactive substances in the liver showed that LPBNSH largely suppressed the formation of these oxidative products at same concentrations. No difference in the abnormal accumulation of copper in the liver between the LPBNSH administered and control groups was observed. From these results, it was concluded that LPBNSH exhibited liver-protective effects against fulminant hepatitis with jaundice at ca. 1/1000, 500 the molar concentration of PBN and, therefore, was clinically promising. [source] Mechanistic Study of the Reaction of Thiol-Containing Enzymes with ,,,-Unsaturated Carbonyl Substrates by Computation and ChemoassaysCHEMMEDCHEM, Issue 6 2010Alexander Paasche Abstract We investigated the reactions between substituted ,,,-unsaturated carbonyl compounds (Michael systems) and thiols by computations as well as chemoassays. The results give insight into variations in the underlying mechanisms as a function of the substitution pattern. This is of interest for the mechanisms of inhibition of the SARS coronavirus main protease (SARS-CoV Mpro) by etacrynic acid derivatives as well as for the excess toxicity of substituted ,,,-unsaturated carbonyl compounds. This study compares possible reaction courses including 1,4-addition followed by a ketonization step, and underscores the importance of a base-catalyzed step for the reactivity of thiol groups in enzymes. Phenyl and methyl substituents at the Michael system decrease the reactivity of the electrophilic compound, but chlorophenyl substituents partly recover the reactivity. Computations also indicate that electron-pushing substituents lead to a change in the reaction mechanism. The conformation of the Michael system is also found to significantly influence reactivity: the s - cis conformation leads to higher reactivity than the s - trans conformation. The computed data explain the trends in measured inhibition potencies of substituted ,,,-unsaturated carbonyl compounds and of reaction rates in chemical assays. They also indicate that the reversibility of inhibition does not stand in contrast to the formation of a new covalent bond between inhibitor and protease. [source] Contact allergy to epoxy (meth)acrylatesCONTACT DERMATITIS, Issue 1 2009Kristiina Aalto-Korte Background: Contact allergy to epoxy (meth)acrylates, 2,2-bis[4-(2-hydroxy-3-methacryloxypropoxy) phenyl]propane (bis-GMA), 2,2-bis[4-(2-hydroxy-3-acryloxypropoxy)phenyl]-propane (bis-GA), 2,2-bis[4-(methacryl-oxyethoxy)phenyl] propane (bis-EMA), 2,2-bis[4-(methacryloxy)phenyl]-propane (bis-MA), and glycidyl methacrylate (GMA) is often manifested together with contact allergy to diglycidyl ether of bisphenol A (DGEBA) epoxy resin. Objective: To analyse patterns of concomitant allergic reactions to the five epoxy (meth)acrylates in relation to exposure. Methods: We reviewed the 1994,2008 patch test files at the Finnish Institute of Occupational Health (FIOH) for reactions to the five epoxy (meth)acrylates, and examined the patients' medical records for exposure. Results: Twenty-four patients had an allergic reaction to at least one of the studied epoxy (meth)acrylates, but specific exposure was found only in five patients: two bis-GMA allergies from dental products, two bis-GA allergies from UV-curable printing inks, and one bis-GA allergy from an anaerobic glue. Only 25% of the patients were negative to DGEBA epoxy resin. Conclusions: The great majority of allergic patch test reactions to bis-GMA, bis-GA, GMA and bis-EMA were not associated with specific exposure, and cross-allergy to DGEBA epoxy resin remained a probable explanation. However, independent reactions to bis-GA indicated specific exposure. Anaerobic sealants may induce sensitization not only to aliphatic (meth)acrylates but also to aromatic bis-GA. [source] Synthesis and structural conformation of N-substituted 1,4-dihyropyridine derivativesCRYSTAL RESEARCH AND TECHNOLOGY, Issue 1 2006M. Mahendra Abstract N-(Phenyl)-3,5-dicarbethoxy-2,6-dimethyl-4-(phenyl)-1,4-dihydropyridine (A) and N-(4-methoxy phenyl)--3,5 dicarbethoxy-2,6 dimethyl-4-(3-nitro phenyl)-1,4-dihydropyridine (B) has been synthesized as per scheme and characterized by the X-ray diffraction method. The compound A crystallizes in monoclinic space group P21/c with cell parameters a = 9.2770(11)Å, b = 8.6410(5)Å, c = 27.601(3)Å, , = 97.724(3)°, Z = 4. The compound B crystallizes in monoclinic space group P21/c with cell parameters a = 11.229(6), b = 12.746(7)Å, c =17.606(6)Å, , = 104.531(3)°, Z = 4. The structures exhibit both intra and intermolecular hydrogen bonds. Dihydropyridine ring of both the compounds adopt a flat boat conformation. (© 2005 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim) [source] Development of fluridil, a topical suppressor of the androgen receptor in androgenetic alopeciaDRUG DEVELOPMENT RESEARCH, Issue 3 2003Allen L Seligson Abstract Nonsteroidal antiandrogens (AA) cannot be topically used for androgenetic alopecia (AGA) because of systemic resorption. A new class of androgen receptor (AR) suppressors designed for safe topical treatment of AGA was synthesized from (3-amino-2-hydroxy-2-methyl- N -(4-nitro-3-trifluoromethyl)phenyl) propanamide (BP-34), to contain perfluoroalkyl moieties. The trifluoromethyl derivative (fluridil) at 10 ,M decreased expression of the AR in LNCaP human cells by 95%, its serum half-life was 6 h; it decomposes hydrolytically to BP-34 and trifluoroacetic acid. Acute intraperitoneal maximum tolerated dose (MTD) of fluridil in mice is 270,300 mg/kg/d and the subacute MTD is 450 mg/kg/d. The oral LD50 in mice was 2,872 mg/kg in males, 2,232 mg/kg in females, and >2,500 mg/kg in rats. Fluridil solution in isopropanol was not cutaneously absorbed in rabbits, did not sensitize or show any phototoxic or photoallergic effects on guinea pig skin, and demonstrated no skin irritation potential in rabbits and humans. Fluridil solid induced only slight and reversible eye irritancy in rabbits and displayed no cytotoxicity to rabbit corneal fibroblasts in vitro. Fluridil demonstrated no significant mutagenicity potential by Ames method. In a double-blind study, 43 males with AGA, Norwood grade II to Va, used topical 2% fluridil in isopropanol or the vehicle daily for 12 months. Anagens (growing hairs) increased in the fluridil group from 76% to 89%. All hematological and biochemistry values remained within normal range, including testosterone, which varied but seasonally. No fluridil or its decomposition product (BP-34) was detected in serum. No adverse side effects were reported. Drug Dev. Res. 59:292,306, 2003. © 2003 Wiley-Liss, Inc. [source] Pharmacodynamics and pharmacokinetics of YM128, a GPIIb/IIIa antagonist prodrugDRUG DEVELOPMENT RESEARCH, Issue 3 2002Ken-ichi Suzuki Abstract We examined the biochemical properties of YM-57029 ({4-[4-(4-Carbamimidoylphenyl)-3-oxopiperazin-1-yl]piperidino}acetic acid monohydrochloride trihydrate) and the pharmacodynamics and pharmacokinetics of its prodrug, YM128 (Ethyl (Z)-(4-{4-[4-(N2 -hydroxycarbamimidoyl)phenyl]-3-oxopiperazin-1-yl}piperidino)acetate), an orally-active glycoprotein IIb/IIIa (GPIIb/IIIa) antagonist. YM-57029 strongly inhibited aggregation of human platelets induced by various agonists, with IC50 values ranging from 3.6 to 51 nM. YM-57029 specifically inhibited fibrinogen binding to purified GPIIb/IIIa about 1,000-fold more potently than Arg-Gly-Asp-Ser (RGDS). Moreover, YM-57029 effectively inhibited an Arg-Gly-Asp (RGD) peptide binding to platelets, suggesting that YM-57029 competed with the RGD sequence of ligand. YM-57029 or YM128 dose-dependently inhibited ex vivo platelet aggregation after iv bolus injection or oral administration to beagle dogs and cynomolgus monkeys. However, YM128 exerted more potent and prolonged inhibitory effects on platelet aggregation than YM-57029 after oral administration to cynomolgus monkeys. Furthermore, YM-57029 prolonged template bleeding time at a dose that inhibited ex vivo platelet aggregation during cumulative iv infusion to cynomolgus monkeys. Metabolic and pharmacokinetic studies showed that YM128 effectively converted into YM-57029 in liver microsomes from humans as well as dogs and monkeys, and that bioavailabilities of YM128 in dogs and monkeys were 32.3 and 22.2%, respectively. These results suggest that YM128, a prodrug of YM-57029, may be a valuable GPIIb/IIIa antagonist with good bioavailability in humans. Drug Dev. Res. 55:149,161, 2002. © 2002 Wiley-Liss, Inc. [source] Asymmetrical Schiff Bases as Carriers in PVC Membrane Electrodes for Cadmium (II) IonsELECTROANALYSIS, Issue 8 2005Hossein Mashhadizadeh, Mohammad Abstract 5-[((4-Methyl phenyl) azo)- N -(6-amino-2-pyridin) salicylaldimine] (S1), and 5-[((4-methyl phenyl) azo)- N -(2-diamino-2-cyano-1-ethyl cyanide) salicylaldehyde] (S2) with N and O donor atoms are effective ionophores to make Cd2+ -selective membrane electrodes. The electrodes based on S1 and S2 exhibits a Nernstian or near-Nernstian response for cadmium ion over a wide concentration range 1.5×10,1,7.5×10,7 with a slope of 28 and 2.0×10,1,4.0×10,7 with a slope of 22, respectively. They have quick response and can be used for three or four months without any divergence in potential. The proposed sensors show fairly good selectivity over some alkali, alkaline earth, transition and heavy metal ions. The electrodes based on S1 and S2 can be used in the pH range 3.5,9. These electrodes were used as an indicator electrode in potentiometric titration of cadmium ion with EDTA and in the direct determination of cadmium ion in aqueous solutions. [source] | |||||||||||||||||||||||||||||||||||||||||||