Pharmacological Characterization of Some Selected 4,5-Dihydro-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates and 3-Hydroxyquinazoline-2,4-diones as (S)-2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)-propionic Acid Receptor Antagonists
نویسندگان
چکیده
منابع مشابه
Synthesis and biological evaluation of novel 9-heteroaryl substituted 7-chloro-4,5-dihydro-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates (TQX) as (R,S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptor antagonists.
In this paper, we report a study on some new 4,5-dihydro-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylate derivatives (TQXs), bearing a nitrogen-containing heterocycle at position-9, and designed as (R,S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptor antagonists. These compounds ensue from the structural modification of previously reported 8-heteroaryl-TQXs which...
متن کامل3D-QSAR studies for the binding affinity toward (R, S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)-propionic acid receptor.
An approach for binding affinity evaluation is suggested and exemplified using a set of triazolo [1,5-a] quinoxaline for the (R, S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)-propionic acid (AMPA) receptor. Biological activity toward the AMPA receptor (expressed as -log IC50) was taken as a dependent variable for building Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular S...
متن کاملSynthesis and Antibacterial Evaluation of (S,Z)-4-methyl-2-(4-oxo-5- ((5-substituted phenylfuran-2-yl) methylene)-2-thioxothiazolidin-3-yl) Pentanoic Acids
The resistance of antimicrobials has become a global hazard with the irrational use of antibiotics. Infection of drug-resistance bacteria seriously threatens human health. Currently there is an urgent need for the development of novel antimicrobial agents with new mechanisms and lower levels of toxicity. In this paper, a series of (S,Z)-4-methyl-2-(4-oxo-5-((5-substitutedphenylfuran-2-yl) methy...
متن کاملSynthesis and Antibacterial Evaluation of (S,Z)-4-methyl-2-(4-oxo-5- ((5-substituted phenylfuran-2-yl) methylene)-2-thioxothiazolidin-3-yl) Pentanoic Acids
The resistance of antimicrobials has become a global hazard with the irrational use of antibiotics. Infection of drug-resistance bacteria seriously threatens human health. Currently there is an urgent need for the development of novel antimicrobial agents with new mechanisms and lower levels of toxicity. In this paper, a series of (S,Z)-4-methyl-2-(4-oxo-5-((5-substitutedphenylfuran-2-yl) methy...
متن کاملSYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 3-(2’-n-BUTYLBENZOFURAN-3’-YL)-5-ARYL-4, 5-DIHYDRO-1H-PYRAZOLES.
3-(2’-n-butylbenzofuran-3’-yl)-5-aryl-4, 5-dihydro-1H-pyrazoles (4a-4k) have been synthesized. The synthesized products have been assayed for their antimicrobial activity against Gram+ve, Gram-ve bacteria and fungi. All the synthesized products were assigned with IR, 1HNMR, Mass Spectra, TLC, and elemental analysis. Some of the products showed moderate activi...
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ژورنال
عنوان ژورنال: Chemical and Pharmaceutical Bulletin
سال: 2010
ISSN: 0009-2363,1347-5223
DOI: 10.1248/cpb.58.908