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New Derivatives (new + derivative)
Selected AbstractsChemInform Abstract: Synthesis and Determination of Acute and Chronic Pain Activities of 1-[1-(3-Methylphenyl)(tetralyl)]piperidine (I) as a New Derivative of Phencyclidine via Tail Immersion and Formalin Tests.CHEMINFORM, Issue 32 2010Abbas Ahmadi No abstract is available for this article. [source] XNA, (xylo Nucleic Acid): A Summary and New DerivativesEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 11 2005B. Ravindra Babu Abstract Fully modified homopyrimidine 2'-deoxy- xylo nucleic acid (dXNA) form triple helixes with complementary DNA/RNA with thermal stabilities comparable to those of the corresponding DNA:DNA and DNA:RNA duplexes. However, a single or few insertions of dXNA monomers in a DNA strand significantly lower duplex stabilities. The dXNA monomers are known to adopt predominantly an N -type furanose conformation in solution. With a desire to increase the binding affinity, seven sugar-modified XNA monomers (H, F, N, M, K, P and Q) have been synthesised and their effect on hybridization towards DNA and RNA complements studied. The introduction of 2'-fluoro and 2'-hydroxy substituents was expected to induce conformational restriction towards C3'- endo -type furanose conformation of monomer F derived from 1-(2'-deoxy-2'-fluoro-,- D -xylofuranosyl)thymine and monomer H derived from 1-(,- D -xylofuranosyl)thymine. The presence of functionalites facing the minor groove as in 1-(2'-amino-2'-deoxy-2'- N,4'- C -methylene-,- D -xylofuranosyl)thymine (monomer N), 1-[4- C -(N -methylpiperazinyl)methyl-,- D -xylofuranosyl]thymine (monomer P), 1-(4- C -piperazinylmethyl-,- D -xylofuranosyl)thymine (monomer Q), 1-(4- C -hydroxymethyl-,- D -xylofuranosyl)thymine (monomer M) and 9-(4- C -hydroxymethyl-,- D -xylofuranosyl)adenine (monomer K) was studied, with monomer N being locked in an N -type furanose conformation. Besides, an efficient synthesis of known xylo -LNA phosphoramidite 19, required for the incorporation of 1-(2'- O,4'- C -methylene-,- D -xylofuranosyl)thymine (monomer L) is described. For comparison, hydridization data of various XNAs reported in the literature are included in the discussion section. The thermal denaturation studies show that XNAs containing conformationally locked monomers (N and L) display improved binding affinity, and that partially modified DNA/XNA chimera, or fully modified XNA display preferential hybridization towards RNA complements. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005) [source] ChemInform Abstract: New Derivatives of 2-(3,5-Dioxo-4-azatricyclo [5.2.1.02,6-endo]dec-8-en-4-yl)acetic Acid.CHEMINFORM, Issue 10 2008Reactivity., Synthesis 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] Synthesis of New Derivatives of Thieno[2,3-b]pyridine Fused with Octyl Ring.CHEMINFORM, Issue 39 2007Fatima A. Al-Omran 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 of New Derivatives of 5,6,7,8-Tetrahydro-1,6-naphthyridines and Their Pharmacological Properties.CHEMINFORM, Issue 2 2006S. Z. Vatsadze Abstract For Abstract see ChemInform Abstract in Full Text. [source] New Derivatives of 3,4-Polymethylene-1,2,4-benzothiadiazine S,S-Dioxides.CHEMINFORM, Issue 2 2006K. G. Nazarenko Abstract For Abstract see ChemInform Abstract in Full Text. [source] Utilization of Hypervalent Iodine in Organic Synthesis: A Novel and Facile Two-Step Protocol for the Synthesis of New Derivatives of 1H-Imidazo[1,2-b]pyrazole by the Cyclocondensation Involving ,-Tosyloxyacetophenones.CHEMINFORM, Issue 32 2005Ming Li No abstract is available for this article. [source] Hypervalent Iodine in Synthesis: A Novel Two-Step Procedure for the Synthesis of New Derivatives of 1H-Imidazo[1,2-b]pyrazole by the Cyclocondensation Between 5-Amino-4-cyano-3-phenyl-1H-pyrazole and ,-Tosyloxyacetophenones or ,-Haloacetophenones.CHEMINFORM, Issue 30 2005Ming Li Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Synthesis and in vitro Cytotoxic Evaluation of New Derivatives of Pyrido[1,2-a]benzimidazolic Ring System: The Pyrido[1,,2,:1,2]imidazo[4,5-h]quinazolines.CHEMINFORM, Issue 7 2002Marianne Dupuy 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] New derivatives of dibenzo[b,e][1,4]diazepin-1-ones by an efficient synthesis and spectroscopyJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 1 2007Eduardo Cortés Cortés An efficient synthesis of four steps to obtain twelve new derivatives of 3,3-dimethyl-2,3,4,5,10,11-hexahydro-8-[(o -; and p -methoxy)phenoxy]-11-[(o -; and p -R)phenyl]-1H -dibenzo[b,e][1,4]diazepin-1-ones IV, 1-12 with possible biological and pharmacological activity as anticonvulsant and schizophrenia treatment in the central nervous system (CNS). The final products were obtained by condensation and cyclization between 3-{4-[(o -; and p -methoxy)phenoxy]-1,2-phenylenediamine}-5,5-dimethyl-2-cyclohexenone with (o -; and p -R)benzaldehyde. The structure of all products was corroborated by spectroscopy of ir, 1H-nmr, 13C-nmr, with bidimensional experiments and MS in Low and high resolution with Collision-Induced Dissociation experiments (CID). [source] Novel Thiophenes, Thienopyrimidines, and Triazolothienopyrimidines for the Evaluation of Anticancer and Augmentation Effects of ,-RadiationARCHIV DER PHARMAZIE, Issue 7 2010Mohamed A. Shaaban Abstract New derivatives of thiophenes 2, 12, iminoaminothieno[2,3- d]pyrimidines 3, 5, and 6, triazolothieno[2,3- d]pyrimidines 8,11, pyrazolo- and triazinothieno[2,3- d]pyrimidines 4, 7, respectively, have been prepared by different synthetic procedures. Structure elucidation of the newly synthesized compounds was carried out via elemental analyses and spectral data. The antitumor activity of compounds 2, 3, and 9,12 was evaluated against in-vitro cell lines (HEPG-2 and MCF-7). Compounds 2, 3, 10, 11, and 12 showed significant in-vitro cytotoxic activity against hepatocellular carcinoma (HEPG-2) compared to the reference drug Doxorubicin. Compound 2 showed significant in-vitro cytotoxic activity against breast cancer (MCF-7) cells compared to the reference drug Doxorubicin. The augmenting effect of ,-radiation was assessed; here, compounds 2, 3, 10, and 11 showed the most potent in-vitro anticancer activity. [source] Quinaphos and Dihydro-Quinaphos Phosphine,Phosphoramidite Ligands for Asymmetric HydrogenationCHEMISTRY - A EUROPEAN JOURNAL, Issue 25 2010Thomas Pullmann Dr. Abstract New derivatives of the Quinaphos ligands and the related Dihydro-Quinaphos ligands based on the more flexible 1,2,3,4-tetrahydroquinoline backbone have been prepared and fully characterised. A general and straightforward separation protocol was devised, which allowed for the gram-scale isolation of the Ra,Sc and Sa,Rc diastereomers. These new phosphine,phosphoramidite ligands have been applied in the Rh-catalysed asymmetric hydrogenation of functionalised olefins with the achievement of excellent enantioselectivities (,99,%) in most cases and turnover frequency (TOF) values of up to ,20,000,h,1. These results substantiate the practical utility of readily accessible Quinaphos-type ligands, which belong to the most active and selective category of ligands for Rh-catalysed hydrogenation known to date. [source] Benzo[d]isothiazol-3-yl-benzamidines: a Class of Protective Agents on Culture of Human Cartilage and Chondrocytes Stimulated by IL-1,CHEMMEDCHEM, Issue 1 2007Paola Vicini Prof. Abstract New derivatives of N -benzo[d]isothiazol-3-yl-benzamidine 6,a were synthesized as nonacidic anti-inflammatory/antidegenerative agents. We investigated the influence of the amidines 6,a,j on the production of NO, PGE2, MMP-3, COX-2, ROS, and GAGs, key molecules involved in cartilage destruction in osteoarthritic diseases. The antidegenerative properties of the novel designed derivatives 6,b,j were improved with respect to N -benzo[d]isothiazol-3-yl-benzamidine 6,a. All of the compounds 6,a,j promoted the reduction of most of the IL-1,-induced harmful effects. Derivatives 6,d, 6,h, and 6,j were the most potent of all the tested compounds, particularly in the human chondrocyte culture model. [source] Influence of lipophilicity and stereochemistry at the C7 position on the cardioprotective and antioxidant effect of ginkgolides during rat heart ischemia and reperfusion,DRUG DEVELOPMENT RESEARCH, Issue 3 2005Ludovic Billottet Abstract The extent to which the cardioprotective effect of ginkgolides is related to their lipophilicity rather than to their anti-platelet activating factor (PAF) effect was addressed in isolated rat hearts submitted to ischemia and reperfusion. A new derivative of ginkgolide C (1), the 7-,- O -(4-methylphenyl) ginkgolide C (4) was synthesized and compared to 7- O -(4-methylphenyl) ginkgolide C (2) that had the same absolute configuration at C7 as 1 for its lipophilicity, anti-PAF activity, and cardioprotective and antioxidant effects. Using reversed-phase high-performance liquid chromatography HPLC, 4 and 2 were found to be significantly more lipophilic (i.e., log kw of 3.42±0.05 and 3.64±0.07, respectively) than 1 (1.15±0.03) and the strong PAF inhibitor ginkgolide B (GkB; 1.65±0.03). The anti-PAF activities (IC50 values in ,M) were 8.2, 17.1, and 2.2 for 4, 1, and GkB, respectively, while 2 was inactive. In preischemic and/or reperfused hearts perfused with ginkgolides at 0.7 ,M: (i) 2 and 4 were more efficient in improving postischemic hemodynamic and metabolic recovery than 1, (ii) a key-step in cardioprotection occurred during ischemia where 2 and 4 limited myocardial ATP depletion and contracture development, (iii) a strong anti-lipoperoxidant effect was observed with 2 and 4, but not 1. In vivo administration of 2 to rats (4 mg/kg/day for 20 days) was more effective than that of 1 regarding ischemic heart protection, suggesting a positive role for lipophilicity. It was concluded that a high lipophilicity is not an absolute prerequisite for a strong anti-PAF effect for ginkgolides, whereas it appears essential for cardioprotection. Drug Dev. Res. 64:157,171, 2005. © 2005 Wiley-Liss, Inc. [source] Fluorescent proteins for single-molecule fluorescence applicationsJOURNAL OF BIOPHOTONICS, Issue 1 2008Britta Seefeldt Abstract We present single-molecule fluorescence data of fluorescent proteins GFP, YFP, DsRed, and mCherry, a new derivative of DsRed. Ensemble and single-molecule fluorescence experiments proved mCherry as an ideally suited fluorophore for single-molecule applications, demonstrated by high photostability and rare fluorescence-intensity fluctuations. Although mCherry exhibits the lowest fluorescence quantum yield among the fluorescent proteins investigated, its superior photophysical characteristics suggest mCherry as an ideal alternative in single-molecule fluorescence experiments. Due to its spectral characteristics and short fluorescence lifetime of 1.46 ns, mCherry complements other existing fluorescent proteins and is recommended for tracking and localization of target molecules with high accuracy, fluorescence resonance energy transfer (FRET), fluorescence lifetime imaging microscopy (FLIM), or multicolor applications. (© 2008 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim) [source] Total assignments of 1H and 13C NMR spectra of isocatalpanol and a derivative of tecomaquinoneMAGNETIC RESONANCE IN CHEMISTRY, Issue 7 2005Allana Kellen L. Santos Abstract Isocatalpanol and tecomaquinone I were obtained from roots of Lippia sidoides, a medicinal plant from northeast Brazil. Reduction of tecomaquinone I with NaBH4 yielded a new derivative. Structural elucidation was done on the basis of spectral data, mainly by high-field NMR and electron ionization mass spectrometry. Copyright © 2005 John Wiley & Sons, Ltd. [source] Investigation of defects in organic semiconductors by charge based Deep Level Transient Spectroscopy (Q-DLTS)PHYSICA STATUS SOLIDI (C) - CURRENT TOPICS IN SOLID STATE PHYSICS, Issue 8 2009T. P. Nguyen Abstract We report the results of measurements of traps in light emitting devices using a new derivative of poly(phenylene vinylene) (PPV) as an active material by the charge based Deep Level Transient Spectroscopy (Q-DLTS) technique. Diodes of structure Indium Tin Oxide (ITO)/PEDOT:PSS/poly(2-ethylhexyl)surfanyl-5-methoxy phenylene vinylene (MEH-S-PPV)/M with M = Al and M = Ca/Al were investigated by measurements of current-voltage-luminance characteristics. From analysis of these characteristics, evidence of charge trapping in devices was demonstrated. The trap parameters were then determined from Q-DLTS measurements, which were carried out on the samples as a function of the charging time, the applied voltage and the temperature. Five trap levels of activation energy in the range [0.3-0.6 eV] and of density of order of 1017 cm,3 were identified in diodes with Ca/Al cathode. Electron (one level) and hole (four levels) traps were then clearly distinguished by performing measurements in hole-only devices. Trapping processes are discussed and tentatively proposed to performance of the light emitting diodes studied. (© 2009 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim) [source] Design and Synthesis of a Gossypol Derivative with Improved Antitumor ActivitiesARCHIV DER PHARMAZIE, Issue 4 2009Yonghua Zhan Abstract A novel chemical process has been devised for the synthesis of a new derivative of gossypol, 6,7,6,,7,-tetrahydroxy-5,5,-diisopropyl-3,3,-dimethyl-[2,2']binaphthalenyl-1,4,1,,4,-tetraone (Apogossypolone). This new process has only four steps, with a shorter synthesis span, a simple purification process, and improved yield and quality. The structure of apogossypolone was characterized by 1H-nuclear magnetic resonance, 13C-nuclear magnetic resonance, mass spectroscopy, infrared spectroscopy, and elemental analysis. Cell-cytotoxicity assay demonstrates that apogossypolone is three- to six-fold more potent than the parent compound, (,)-gossypol, in inhibiting the human prostate tumor cell lines PC-3 and DU-145 as well as the human breast cancer cell line MDA-MB-231. The colony-formation assay with DU-145 cells showed that apogossypolone inhibited more than 70% of colony formation at 1 ,M, whereas (,)-gossypol at 10 ,M only inhibited less than 50% of colony formation. The results indicate that apogossypolone exerts strong antitumor activities in human prostate and breast cancer cells, and thus represents a promising cancer therapeutic. [source] Multinuclear magnetic resonance, electrospray ionization,mass spectroscopy, and parametric method 5 studies of a new derivative of gossypol with 2-thiophenecarbohydrazide as well as its complexes with LI+, Na+, K+, RB+, and Cs+ cationsBIOPOLYMERS, Issue 3 2006Piotr Przybylski Abstract A new derivative of racemic gossypol with 2-thiophenecarbohydrazide (GHHT) and its complexes with monovalent cations have been synthesized and studied by electrospray ionization,mass spectroscopy (ESI-MS), multinuclear nuclear magnetic resonance (NMR), as well as by the Parametric Method 5 (PM5) methods. It is demonstrated that GHHT forms stable complexes of 1:1 stoichiometry with monovalent metal cations. The structures of the complexes are stabilized by three types of intramolecular hydrogen bonds. The spectroscopic methods have provided clear evidence that GHHT and its complexes exist in the DMSO-d6 solution in the N-imine,N-imine tautomeric forms. The structures of the GHHT and its complexes with Li+, Na+, K+, Rb+, and Cs+ cations are visualized and discussed in detail. © 2006 Wiley Periodicals, Inc. Biopolymers 83: 213,225, 2006 This article was originally published online as an accepted preprint. The "Published Online" date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com [source] Synthesis and Structural Characterization of 1,4-Di(2-methoxyphenyl)-2,5-piperazinedioneCHINESE JOURNAL OF CHEMISTRY, Issue 5 2007Shu-Sheng Zhang Abstract A new derivative of 2,5-piperazinedione, 1,4-di(2-methoxyphenyl)-2,5-piperazinedione (I), was synthesized by the cyclocondensation reaction of N -2-methoxyphenyl chloroacetamide, and its structure was characterized by elemental analysis, IR, 1H NMR and single crystal X-ray diffraction method. The crystal belongs to monoclinic system, space group P21/c with unit cell dimensions a=0.56934(10) nm, b=1.3880(2) nm, c=1.00329(17) nm, ,=90.376(3)°, V=0.7928(2) nm3, Z=2, Dc=1.367 g·cm,3, ,=0.98 cm,1, R and wR being 0.0606 and 0.1564 respectively for 1549 unique reflections with 1247 observed reflections [I>2,(I)]. The molecule has a crystallographically imposed symmetry center. The three rings in the molecule are each coplanar with their attached groups, excluding methyl H atoms and the H atoms attached to the piperazinedione ring, while the whole molecule is not planar, with dihedral angles of 74.7(1)° between the piperazinedione and each of the two aromatic rings. The crystal structure is stabilized by van der Waals and dipole-dipole forces. [source] Self-Organization of Dipolar 4,4,-Disubstituted 2,2,-Bipyridine Metal Complexes into Luminescent Lamellar Liquid CrystalsEUROPEAN JOURNAL OF INORGANIC CHEMISTRY, Issue 19 2003Daniela Pucci Abstract Mononuclear cis -dichloro complexes, [LnMCl2], with different metal centres (PtII, NiII, and ZnII) and a series of palladium and platinum derivatives, [L2MX2], in which chloride groups are replaced with iodide, bromide, and azide ligands, have been synthesized from 4,4,-disubstituted-2,2,-bipyridines. Upon complexation of these non-mesogenic ligands, the peculiar structural arrangement, characterized by intermolecular associations of the new derivatives, induces mesomorphism in most [L2MX2] complexes, confirming the importance of coordination chemistry in metal-mediated formation of liquid crystals. Single crystal X-ray structures have been determined for dihexadecyl 2,2,-bipyridyl-4,4,-dicarboxylatopalladium and -zinc dichloride derivatives. Both the metal centres and the ancillary ligands have been varied to use dipole coupling as a tool to control molecular architecture: thermal, as well as spectroscopic properties, depend strongly upon molecular dipolar interactions. Tunable red and blue emitters based on PdII and PtII, both in solution and in the solid state, have been obtained. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003) [source] Stable Ion and Electrophilic Substitution (Nitration and Bromination) Study of A-Ring Substituted Phenanthrenes: Novel Carbocations and Substituted Derivatives; NMR, X-ray Analysis, and Comparative DNA BindingEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 3 2007Cédric Brulé Abstract Persistent carbocations were generated from five A-ring mono- and di-substituted phenanthrenes [3-OMe; 4-OMe, 1,3-bis(OMe), 2,4-bis(OMe), and 1,3-bis(Me)]. In all cases protonation occurs in the A-ring, ortho/para relative to methoxy or methyl substituent(s). Complete NMR assignments of the resulting carbocations are reported and their charge delocalization modes are discussed. Mild nitration (with 20,50,% aqueous HNO3 at ,10 °C or at room temp.) and bromination (NBS/MeCN/room temp.) of these substrates resulted in the synthesis of several novel mononitro-/dinitro- as well as monobromo/dibromo derivatives, including those with nitro or bromo substituent in the bay-region. Correspondence between the site of attack in low-temperature protonation study and nitro substitution in ambient mild nitrations are examined. Complete NMR assignments for the new derivatives are reported as well as X-ray structures for 2,4-dimethoxy-1-nitro- and 1,3-dimethyl-4-nitrophenanthrenes. A comparative DNA binding study with MCF cells on three of the synthesized mononitro and one dinitro derivative showed that 1,3-dimethyl-9-nitro- (nitro at the meso position), 3-methoxy-4-nitro- (nitro in bay-region), and 1,3-dimethoxy-4,9-dinitrophenanthrenes (nitro in both meso and bay-regions) formed DNA adducts. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2007) [source] Synthesis of Pyrazolyl-2-pyrazolines by Treatment of 3-(3-Aryl-3-oxopropenyl)chromen-4-ones with Hydrazine and Their Oxidation to Bis(pyrazoles)EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 22 2004Albert Lévai Abstract The synthesis of several 1-acetyl-3-aryl-5-[3-(2-hydroxyphenyl)pyrazol-4-yl]-2-pyrazolines 3a,3h has been accomplished by treatment of the 3-(3-aryl-3-oxopropenyl)chromen-4-ones 1a,h with hydrazine hydrate in hot acetic acid. The 1-acetyl-3-aryl-5-(3-chromonyl)-2-pyrazolines 2a,2f were also obtained as by-products. Oxidation of the 1-acetyl-4-pyrazolyl-2-pyrazolines 3a,3f with DDQ gave the 3(5)-aryl-5(3)-[3-(2-hydroxyphenyl)pyrazol-4-yl]pyrazoles 5a,5f. The oxidation of the 2-pyrazoline rings was accompanied by N -deacylation. The reaction mechanisms of both transformations are discussed, the first one being supported by experimental results. The structures of all new derivatives were established by NMR and the evidence of prototropic tautomerism is carefully discussed. Theoretical calculations of energies and of the 1H and 13C NMR chemical shifts of the possible tautomeric forms of 5(3)-[3-(2-hydroxyphenyl)pyrazol-4-yl]-3(5)-(4-methoxyphenyl)pyrazole (5c), by B3LYP and GIAO, showed that compounds of this type probably exist as mixtures of two tautomers. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004) [source] 3(5)-(2-Hydroxyphenyl)-5(3)-styrylpyrazoles: Synthesis and Diels,Alder TransformationsEUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Issue 21 2004Vera L. M. Silva Abstract Reactions between cinnamoyl(2-hydroxybenzoyl)methanes and hydrazine hydrate in acetic acid gave 3-(2-hydroxyphenyl)-5-styrylpyrazoles, while the corresponding reactions with phenylhydrazine yielded 5-(2-hydroxyphenyl)-1-phenyl-3-styrylpyrazoles as the major products and 3-(2-hydroxyphenyl)-1-phenyl-5-styrylpyrazoles as by-products. The reaction mechanism of this transformation is discussed. The first cycloaddition reactions between ortho -benzoquinodimethane and either 3-(2-hydroxyphenyl)-5-styrylpyrazoles or 5-(2-hydroxyphenyl)-1-phenyl-3-styrylpyrazoles afforded 5-[2-(3-aryl-1,2,3,4-tetrahydronaphthyl)]-3-(2-hydroxyphenyl)pyrazoles or 3-[2-(3-aryl-1,2,3,4-tetrahydronaphthyl)]-1-phenyl-5-(2-hydroxyphenyl)pyrazoles, respectively. These cycloadducts were converted into the corresponding naphthylpyrazoles by oxidation with DDQ in dry 1,4-dioxane. The structures of all new derivatives have been established by NMR spectroscopy. (© Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004) [source] NMR-Solution Structures and Affinities for the Human Somatostatin G-Protein-Coupled Receptors hsst1,5 of CF3 Derivatives of Sandostatin® (Octreotide)HELVETICA CHIMICA ACTA, Issue 12 2009Dieter Seebach Abstract The previously reported (Helv. Chim. Acta2008, 91, 2035) derivatives of octreotide (1) with a (CF3)-Trp substitution, i.e., 3, and with open-chain structures, i.e., 2, 4, and 5, have been tested for their affinities to hsst1,5 receptors and subjected to a detailed NMR analysis. Their affinities vary from 15,nM to 5,,M, as compared to 0.6,nM to 0.8,,M for octreotide itself (Table,1). This decreased bioactivity may have had to be expected for the open-chain compounds 4 and 5; possible reasons for this decrease in the case of CF3 derivative of octreotide, 3, are discussed. NMR Analysis (Tables,2 and 3) provides evidence for increased dynamics of all new derivatives 2,5. The dynamics of the octreotide molecule 1 was analyzed by (natural-abundance) longitudinal 13C-T1 -relaxation time measurements (Table,4), from which the conclusion is drawn that the backbone of the macrocycle is rather rigid on the time scale of this method. [source] New derivatives of dibenzo[b,e][1,4]diazepin-1-ones by an efficient synthesis and spectroscopyJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 1 2007Eduardo Cortés Cortés An efficient synthesis of four steps to obtain twelve new derivatives of 3,3-dimethyl-2,3,4,5,10,11-hexahydro-8-[(o -; and p -methoxy)phenoxy]-11-[(o -; and p -R)phenyl]-1H -dibenzo[b,e][1,4]diazepin-1-ones IV, 1-12 with possible biological and pharmacological activity as anticonvulsant and schizophrenia treatment in the central nervous system (CNS). The final products were obtained by condensation and cyclization between 3-{4-[(o -; and p -methoxy)phenoxy]-1,2-phenylenediamine}-5,5-dimethyl-2-cyclohexenone with (o -; and p -R)benzaldehyde. The structure of all products was corroborated by spectroscopy of ir, 1H-nmr, 13C-nmr, with bidimensional experiments and MS in Low and high resolution with Collision-Induced Dissociation experiments (CID). [source] Synthesis and antiproliferative evaluation of new aryl substituted pyrido[3,,2,:5,6]thiopyrano[4,3- c]pyrazolesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 7 2005G. Primofiore The preparation and the cytotoxic properties of new derivatives of the planar pyrido[3,,2,:5,6]thiopyrano-[4,3- c]pyrazole system, carrying an arylic side group in the 1 or 2 positions, are described. The novel substituted derivatives were obtained by reaction of suitable arylhydrazines with the appropriate key intermediate 3-hydroxymethylene-2,3-dihydrothiopyrano[2,3- b]pyridin-4(4H)-ones. Moreover the preparation was reported of the 2-carboxamidophenyl derivatives, which was accomplished from the previously obtained pyrido[3,,2,:5,6]thiopyrano[4,3- c]pyrazole nucleus, by reaction with phenylisocyanate. All the new compounds were evaluated for their antiproliferative ability, by an in vitro assay on human tumor cell lines (HL-60 and HeLa). [source] Synthesis and biological effects of new derivatives of benzotriazole as antimicrobial and antifungal agentsJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 5 2002Fatima Al-Omran Derivatives of 2-aminothiophene-3-carbonitrile, 2-thioxopyridine-3-carbonitrile, 1,8-naphthyridine-2-one, thieno[2,3- b]pyridine-5-carbonitrile and thieno[2,3- d]pyrimidine incorporating with a 1H -benzo-triazole moiety or 1,3,4-thiadiazole derivatives incorporating with a benzotriazol-1-ylmethyl group have been synthesized and tested for antimicrobial and antifungal activities. The structures of the newly synthesized compounds have been established on the basis of their analytical and spectral data. [source] Analysis of alcohols, as dimethylglycine esters, by electrospray ionization tandem mass spectrometryJOURNAL OF MASS SPECTROMETRY (INCORP BIOLOGICAL MASS SPECTROMETRY), Issue 3 2001Dr David W. Johnson Abstract Dimethylglycine (DMG) esters are new derivatives for the rapid, sensitive and selective analysis of primary and secondary alcohols, in complex mixtures, by electrospray ionization tandem mass spectrometry (ESI-MS/MS). Their development was inspired by the use of the complementary dimethylaminoethyl esters for the trace, rapid analysis of fatty acids. DMG esters are simply prepared by heating a dichloromethane solution of the imidazolide of dimethylglycine, containing triethylamine, and an alcohol. DMG esters of long-chain fatty alcohols, isoprenoidal alcohols and hydroxy-acids are analysed by electrospray ionization tandem mass spectrometry with a precursor ion of m/z 104 scan. Diols, glyceryl esters, glyceryl ethers and some sterols are analysed by a neutral loss of 103 Da scan. Trimethylglycine (TMG) ester iodides, prepared by alkylation of DMG esters with methyl iodide, are more sensitive derivatives for molecules containing secondary alcohol groups, such as cholesterol and gibberellic acid. They are analysed by a precursor ion of m/z 118 scan. DMG or TMG derivatives were shown to be at least comparable and sometimes an order of magnitude more sensitive than N -methylpyridyl ether derivatives for ESI-MS/MS analysis of the different classes of alcohols. Applications of these derivatives for the diagnosis of inherited disorders and the analysis of natural products are presented. Copyright © 2001 John Wiley & Sons, Ltd. [source] Antimalarial compounds isolated from plants used in traditional medicineJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 11 2009Joanne Bero Abstract Objectives This review covers the compounds with antiplasmodial activity isolated from plants published from 2005 to the end of 2008, organized according to their phytochemical classes. Details are given for substances with IC50 values , 11 ,M. Key findings Malaria is a major parasitic disease in many tropical and subtropical regions and is responsible for more than 1 million deaths each year in Africa. The rapid spread of resistance encourages the search for new active compounds. Nature and particularly plants used in traditional medicine are a potential source of new antimalarial drugs as they contain molecules with a great variety of structures and pharmacological activities. Summary A large number of antimalarial compounds with a wide variety of structures have been isolated from plants and can play a role in the development of new antimalarial drugs. Ethnopharmacological approaches appear to be a promising way to find plant metabolites that could be used as templates for designing new derivatives with improved properties. [source] | ||||||||||||||||||||||||||||||||||