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P1 Receptor Agonists/Antagonists in Clinical Trials - Potential Drug Candidates of the Future.
This review is an attempt to highlight the current status, progress and probable future of P1 receptor ligands which are under clinical trials as promising novel therapeutic agents and the direction in which research should proceed with a view to come out with novel therapeutic agent. Expand
Synthesis, anti-inflammatory evaluation, and docking studies of some new thiazole derivatives
AbstractA series of new 2-substituted-N-(1,3-thiazole-2-yl)acetamide 3–7 and N-(benzo[d]thiazol-2-yl)-2-(substituted)acetamide 10–13 derivatives have been synthesized and evaluated in vivo (rat pawExpand
Synthesis, adenosine receptor binding and molecular modelling studies of novel thieno[2,3‐d]pyrimidine derivatives
A series of new molecules containing a thieno[2,3‐d]pyrimidine scaffold was synthesized and characterized by adopting an efficient synthetic scheme and the role of important amino acid residues for imparting good affinity towards hA3 and hA2A ARs was revealed. Expand
7‐Amino‐2‐aryl/hetero‐aryl‐5‐oxo‐5,8‐dihydro[1,2,4]triazolo[1,5‐a]pyridine‐6‐carbonitriles: Synthesis and adenosine receptor binding studies
Encouraging results for compounds 4a and 4t indicate that substitution at 2‐position of the scaffold with π‐excessive systems other than thiophene may lead to even more potent and selective hA1 AR antagonists. Expand
Synthesis and adenosine receptors binding studies of new fluorinated analogues of pyrido[2,3-d]pyrimidines and quinazolines
A series of new fluorine containing pyrido[2,3-d]pyrimidines and imidazo[1,2-c]pyrido[3,2-e]pyrimidines along with a series of bioisosteric fluorinated quinazolines were synthesised followingExpand
Molecular modeling approaches for the discovery of adenosine A2B receptor antagonists: current status and future perspectives.
This review provides a systematic outline of advances in molecular modeling approaches towards A2BAR for deducing its structure and interactions with various types of antagonist and provides impetus for medicinal chemists to discover potential ligands that can bind selectively with higher affinity to A1BAR. Expand
Current Status in the Design and Development of Agonists and Antagonists of Adenosine A3 Receptor as Potential Therapeutic Agents.
This review shall focus on the medicinal chemistry of the A3AR ligands exploring the diverse chemical classes that have been projected as future lead as drug candidates. Expand
Synthesis of novel 2-alkyl-4-substituted-amino-pyrazolo[3,4-d]pyrimidines as new leads for anti-bacterial and anti-cancer activity
Treatment of 6-alkyl-1-phenyl-4-chloro-(1H)-pyrazolo[3,4-d]pyrimidines, with different amines afforded a series of compounds whose identity and purity were confirmed by spectral and analytical means.Expand
Cytotoxicity and Antimycobacterial Properties of Pyrrolo[1,2-a]quinoline Derivatives: Molecular Target Identification and Molecular Docking Studies
The test compound dimethyl-1-(4-fluorobenzoyl)-5-methylpyrrolo[1,2-a]quinoline-2,3-dicarboxylate 4j emerged as the most promising anti-TB agent against H37Rv and multidrug-resistant strains of Mycobacterium tuberculosis at 8 and 16 µg/mL, respectively. Expand
Protective Effect of A2B Receptor Antagonist (TRP 1) on Acetic Acid Induced Ulcerative Colitis in Rats: in vitro, in vivo and in silico Methods
The data demonstrated that the TRP 1 treatment improved clinical score in acetic acid induced colitis in rats and inhibited the proinflammatory cytokine IL-6, IL 1β and TNF α and improvements of antioxidant in colitis rats through A2B receptor antagonist property. Expand