tetrazoles

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关键词:'tetrazoles'

显示 31-60 共 1566 条结果关于 "tetrazoles" 范围论文

Replacement of the double bond of antitubulin chalcones with triazoles and tetrazoles: Synthesis and biological evaluation.

Ornella Mesenzani et al.

Bioorganic & medicinal chemistry letters, 21(2), 764-768 (2010-12-21)

In the chalcone scaffold, it is thought that the double bond is an important structural linker but it is likely not essential for the interaction with tubulin. Yet, it may be a potential site of metabolic degradation and interaction with

Azole antimicrobial pharmacophore-based tetrazoles: synthesis and biological evaluation as potential antimicrobial and anticonvulsant agents.

Sherif A F Rostom et al.

Bioorganic & medicinal chemistry, 17(6), 2410-2422 (2009-03-03)

The azole pharmacophore is still considered a viable lead structure for the synthesis of more efficacious and broad spectrum antimicrobial agents. Potential antibacterial and antifungal activities are encountered with some tetrazoles. Therefore, this study presents the synthesis and antimicrobial evaluation

Exploration on asymmetric synthesis of flavanone catalyzed by (S)-pyrrolidinyl tetrazole.

Shubao Zhou et al.

Chirality, 23(7), 504-506 (2011-04-19)

An improved method of the synthesis of flavanones catalyzed by pyrrolidine and BF(3) ·Et(2) O has been developed and a lot of flavanones could be easily synthesized via this method. The asymmetric synthesis of flavanone from benzaldehyde and 5-fluoro-2-hydroxyacetophenone has

Structure-property relationships of energetic nitrogen-rich salts composed of triaminoguanidinium or ammonium cation and tetrazole-based anions.

Yuling Shao et al.

Journal of molecular graphics & modelling, 40, 54-63 (2013-01-29)

Density functional theory and volume-based thermodynamics calculations have been performed to study the crystal densities, heats of formation (HOFs), energetic properties, and thermodynamics of formation for a series of ionic salts composed of triaminoguanidinium or ammonium cations and tetrazole-based anions.

The hydrogen bond environments of 1H-tetrazole and tetrazolate rings: the structural basis for tetrazole-carboxylic acid bioisosterism.

Frank H Allen et al.

Journal of chemical information and modeling, 52(3), 857-866 (2012-02-07)

Bioisosterism involving replacement of a carboxylic acid substituent by 1H-tetrazole, yielding deprotonated carboxylate and tetrazolate under physiological conditions, is a well-known synthetic strategy in medicinal chemistry. To improve our overall understanding of bioisosterism, we have used this example to study

Fast-LC determination of 1-methyl-1H-tetrazole-5-thiol in human plasma with column-switching sample clean-up.

P A Bombardt et al.

Journal of pharmaceutical and biomedical analysis, 8(1), 73-77 (1990-01-01)

A simple, fast and sensitive method for the quantitative determination of 1-methyl-1H-tetrazole-5-thiol using HPLC is reported. Samples are deproteinated by plasma water filtration and injected into a HPLC system capable of column switching and backflushing the analytical column. The limit

GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.

Jason E Imbriglio et al.

Bioorganic & medicinal chemistry letters, 19(8), 2121-2124 (2009-03-25)

5-Alkyl and aryl-pyrazole-tetrazoles have been identified as a new class of selective, small-molecule, agonists of the human G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid.

Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors.

Baker Jawabrah Al-Hourani et al.

Bioorganic & medicinal chemistry letters, 22(6), 2235-2238 (2012-02-22)

A series of novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors was prepared via treatment of various diaryl amides with tetrachlorosilane/sodium azide. All compounds were tested in cyclooxygenase (COX) assays in vitro to determine COX-1 and COX-2 inhibitory potency and selectivity.

Photochemistry and vibrational spectra of matrix-isolated 5-ethoxy-1-phenyl-1H-tetrazole.

Luís M T Frija et al.

The journal of physical chemistry. A, 111(15), 2879-2888 (2007-03-29)

A combined matrix isolation FT-IR and theoretical DFT(B3LYP)/6-311++G(d,p) study of the molecular structure and photochemistry of 5-ethoxy-1-phenyl-1H-tetrazole (5EPT) was performed. A new method of synthesis of the compound is described. Calculations show three minima, very close in energy and separated

Retention characteristics of poly(N-(1H-tetrazole-5-yl)-methacrylamide)-bonded stationary phase in hydrophilic interaction chromatography.

Xiaoqing Fu et al.

Journal of chromatography. A, 1609, 460500-460500 (2019-09-14)

A Poly(N-(1H-tetrazole-5-yl)methacrylamide)-bonded (PTZ) stationary phase has recently gained increased attention in hydrophilic liquid chromatography (HILIC) mode for separation of polar compounds and is now commercially available as DCpak PTZ. It is chromatographically characterized in this work. The property of the

A novel one-pot pseudo-five-component condensation reaction towards bifunctional diazepine-tetrazole containing compounds: synthesis of 1H-tetrazolyl-1H-1,4-diazepine-2,3-dicarbonitriles and 1H-tetrazolyl-benzo[b][1,4]diazepines.

Hamid Mofakham et al.

Molecular diversity, 16(2), 351-356 (2012-05-18)

A novel and efficient method has been developed for the one-pot synthesis of bifunctional diazepine-tetrazole containing compounds. 1H-Tetrazolyl-1H-1,4-diazepine-2, 3-dicarbonitrile and 1H-tetrazolyl-benzo[b][1,4]diazepine derivatives were synthesized in good yields using 2,3-diaminomaleonitrile or an aromatic diamine, ketones, trimethylsilyl azide, and an isocyanide in

Synthesis and biological evaluation of new N-acyl-homoserine-lactone analogues, based on triazole and tetrazole scaffolds, acting as LuxR-dependent quorum sensing modulators.

Mohamad Sabbah et al.

Bioorganic & medicinal chemistry, 20(15), 4727-4736 (2012-07-04)

New analogues of N-acyl-homoserine-lactone (AHL), in which the amide was replaced by a triazole or tetrazole ring, were prepared and tested for their activity as LuxR-dependent QS modulators. Several compounds showed a level of antagonistic or agonistic activity, notably some

Polyfunctional tetrazolic thioethers through electrooxidative/Michael-type sequential reactions of 1,2- and 1,4-dihydroxybenzenes with 1-phenyl-5-mercaptotetrazole.

Mohammad M Khodaei et al.

The Journal of organic chemistry, 73(7), 2527-2532 (2008-03-05)

In the presence of 1-phenyl-5-mercaptotetrazole as a nucleophile, electrochemical oxidations of 1,2- and 1,4-dihydroxybenzenes have been investigated in aqueous solution using cyclic voltammetry and controlled-potential coulometry. The voltammetric results indicate that an electrooxidative/Michael-type sequential reaction occurs between the mercaptide anion

A highly specific tetrazole-based chemosensor for fluoride ion: a new sensing functional group based on intramolecular proton transfer.

Ju-Ying Li et al.

Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 102, 66-70 (2012-12-05)

A simple but highly selective colorimetric and fluorescent chemosensor for fluoride ion has been prepared based on coumarin chromophore and 1H-tetrazole. Tetrazole functional group provided a novel sensing functional group containing the ESIPT structure for designing fluoride chemosensor.

Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis.

Kim F McClure et al.

Angewandte Chemie (International ed. in English), 56(51), 16218-16222 (2017-10-27)

Targeting of the human ribosome is an unprecedented therapeutic modality with a genome-wide selectivity challenge. A liver-targeted drug candidate is described that inhibits ribosomal synthesis of PCSK9, a lipid regulator considered undruggable by small molecules. Key to the concept was

Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).

P Douglas Boatman et al.

Bioorganic & medicinal chemistry letters, 20(9), 2797-2800 (2010-04-07)

Tricyclic pyrazole tetrazoles which are potent partial agonists of the high affinity niacin receptor, GPR109a, have been discovered and optimized. One of these compounds has proven to be effective at lowering free fatty acids in vitro and in vivo.

Studies on adsorption of 5-amino tetrazole on silver nanoparticles by SERS and DFT calculations.

S Thomas et al.

The journal of physical chemistry. A, 109(44), 9928-9934 (2006-07-15)

The surface-enhanced Raman scattering (SERS) studies of 5-amino tetrazole (5AT), a tetrazole derivative, in aqueous silver sol at pH approximately 9 and on deposited colloidal silver films were carried out and compared with the normal Raman spectrum of the molecule.

Enzymatic hydrolysis of esters containing a tetrazole ring.

Edyta Łukowska-Chojnacka et al.

Chirality, 26(12), 811-816 (2014-07-30)

The lipase-catalyzed enantioselective hydrolysis of acetates containing tetrazole moiety was studied. Among all tested lipases, Novozyme SP 435 allowed to obtain optically active 4-(5-aryl-2H-tetrazol-2yl)butan-2-ol and 1-(5-aryl-2H-tetrazol-2yl)-propan-2-ol and their acetates with the highest optical purities (ee = 95%-99%) and excellent enantioselectivity (E>100). Some

Cellular membrane contrast and contrast differentiation with osmium triazole and tetrazole complexes.

W C de Bruijn et al.

The Histochemical journal, 16(1), 37-50 (1984-01-01)

Addition of heterocyclic nitrogen compounds to the classical osmium tetroxide postfixation medium, applied after glutaraldehyde fixation, results in enhanced membrane contrast in ultrathin sections of liver tissue. The addition of similar compounds to potassium osmate solutions, results in contrast differences

Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.

Arturo Perez-Medrano et al.

Bioorganic & medicinal chemistry letters, 21(11), 3297-3300 (2011-05-04)

Synthesis and biological evaluation of a novel class of substituted N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine derivatives resulted in the identification of potent P2X(7) antagonists. These compounds were assayed for activity at both the human and rat P2X(7) receptors. On the benzyl moiety, a variety

Metal-free nitrogen-containing carbon nanotubes prepared from triazole and tetrazole derivatives show high electrocatalytic activity towards the oxygen reduction reaction in alkaline media.

Adina Morozan et al.

ChemSusChem, 5(4), 647-651 (2012-03-06)

High-performance oxygen reduction reaction (ORR) catalysts based on metal-free nitrogen-containing precursors and carbon nanotubes are reported. The investigated systems allow the evaluation of the effect of nitrogen-containing groups towards ORR and the results show that the catalysts are compatible with

Crystal engineering of Fe(II) spin crossover coordination polymers derived from triazole or tetrazole ligands.

Yann Garcia et al.

Chimia, 67(6), 411-418 (2013-08-16)

The past decade has witnessed intense research activity in the area of Fe(II) spin crossover coordination polymers, which are structurally diverse and functionally intriguing materials. In this endeavor, a less exploited series of ligands have been selected among various N-donor

Microcin C and albomycin analogues with aryl-tetrazole substituents as nucleobase isosters are selective inhibitors of bacterial aminoacyl tRNA synthetases but lack efficient uptake.

Gaston H Vondenhoff et al.

Chembiochem : a European journal of chemical biology, 13(13), 1959-1969 (2012-08-01)

In 1998, Cubist Pharmaceuticals patented a series of aminoacyl tRNA synthetase (aaRS) inhibitors based on aminoacyl sulfamoyladenosines (aaSAs), in which the adenine was substituted by aryl-tetrazole moieties linked to the ribose fragment by a two-carbon spacer. Although potent and specific

Tuning the framework topologies of Co(II)-doped Zn(II)-tetrazole-benzoate coordination polymers by ligand modifications: structures and spectral studies.

Wei-Chao Song et al.

Inorganic chemistry, 48(8), 3792-3799 (2009-03-24)

In our continuing efforts to explore the effects of ligand modifications on the structures and properties of their metal complexes, we studied the in situ [2 + 3] cycloaddition reactions of benzonitrile, o-phthalodinitrile, 3-cyanobenzoic acid, 4-cyanobenzoic acid with NaN(3) in

Synthesis of tetrazole analogues of phosphonohydroxamic acids: an attempt to improve the inhibitory activity against the DXR.

Anh Thu Nguyen-Trung et al.

Bioorganic & medicinal chemistry letters, 23(6), 1643-1647 (2013-02-19)

This work is focused on the design of new antimicrobial drugs and on the development of lipophilic inhibitors of the DXR, the second enzyme of the MEP pathway for the biosynthesis of isoprene units in most bacteria, by replacing the

Design, synthesis, and biological evaluation of novel hybrid dicaffeoyltartaric/diketo acid and tetrazole-substituted L-chicoric acid analogue inhibitors of human immunodeficiency virus type 1 integrase.

David C Crosby et al.

Journal of medicinal chemistry, 53(22), 8161-8175 (2010-10-28)

Fourteen analogues of the anti-HIV-1 integrase (IN) inhibitor L-chicoric acid (L-CA) were prepared. Their IC(50) values for 3'-end processing and strand transfer against recombinant HIV-1 IN were determined in vitro, and their cell toxicities and EC(50) against HIV-1 were measured

Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole.

Kyriaki Pegklidou et al.

Bioorganic & medicinal chemistry, 18(6), 2107-2114 (2010-03-02)

Pyrrolyl-propionic and butyric-acid derivatives 1 and 2 were synthesized in order to study the effect of the variation of the methylene chain in comparison to the previously reported pyrrolyl-acetic acid compound I, which was found as potent aldose reductase inhibitor

Mechanisms involved in the antinociceptive and anti-inflammatory effects of a new triazole derivative: 5-[1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl]-1H-tetrazole (LQFM-096).

Carina S Cardoso et al.

Inflammopharmacology, 28(4), 877-892 (2020-02-08)

The aim of this study was to design, synthesize and evaluate the potential analgesic and anti-inflammatory effects of 5-[1-(4-fluorphenyl)-1H-1,2,3-triazol-4-yl]-1H-tetrazole-(LQFM-096: a new triazole compound) as well as to elucidate its possible mechanisms of action. The oral administration of LQFM-096 (10, 20

Effect of side chains including the N-methyl-tetrazole-thiol group of beta-lactam antibiotics on transport in cultured kidney epithelial cells LLC-PK1.

K Goto et al.

Biological & pharmaceutical bulletin, 21(10), 1113-1116 (1998-11-20)

In this study, the transcellular transport characteristics of four beta-lactam antibiotics (cefotaxime, cefmenoxime, cefmetazole, and cefotiam) were investigated in a kidney epithelial cell line LLC-PK1, especially focusing on the effect of the N-methyl-tetrazole-thiol (NMTT) group attached to 7-amino-cephalosporanic acid. There

Design, synthesis and biological evaluation of 3-substituted 2,5-dimethyl-N-(3-(1H-tetrazol-5-yl)phenyl)pyrroles as novel potential HIV-1 gp41 inhibitors.

Xiao-Yang He et al.

Bioorganic & medicinal chemistry, 19(22), 6726-6734 (2011-10-22)

Based on the structure of HIV-1 gp41 binding site for small-molecule inhibitors, optimization of lead 2 resulted in the discovery of a new series of 2,5-dimethyl-3-(5-(N-phenylrhodaninyl)methylene)-N-(3-(1H-tetrazol-5-yl)phenyl)pyrrole compounds with improved anti-HIV-1 activity. The most active compounds 13a and 13j exhibited significant

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