Banerjee, Abhisek; Pawar, Mahesh Y.; Patil, Sandip; Yadav, Pravin S.; Kadam, Pradip A.; Kattige, Vidya G.; Deshpande, Durga S.; Pednekar, Pallavi V.; Pisat, Monali K.; Gharat, Laxmikant A. published the artcile< Development of 2-aryl substituted quinazolin-4(3H)-one, pyrido[4,3-d]pyrimidin-4(3H)-one and pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as microsomal prostaglandin E2 synthase-1 inhibitors>, Recommanded Product: 2-Amino-4-bromobenzamide, the main research area is quinazolinone preparation microsomal prostaglandin PGE2 synthase inhibitor NSAID analgesic; pyridopyrimidinone preparation microsomal prostaglandin PGE2 synthase inhibitor NSAID analgesic; Analgesic; Cyclooxygenase; Prostaglandin E(2); Quinazolinone; mPGES-1.
MPGES-1 is inducible terminal synthase acting downstream of COX enzymes in arachidonic acid pathway, regulates the biosynthesis of pro-inflammatory prostaglandin PGE2. Cardiovascular side effect of coxibs and NSAIDs, selective for COX-2 inhibition, stimulated interest in mPGES-1, a therapeutic target with potential to deliver safe and effective anti-inflammatory drugs. The synthesis and structure activity relationship of a series of compounds from 2-aryl substituted quinazolin-4(3H)-one, pyrido[4,3-d]pyrimidin-4(3H)-one and pyrido[2,3-d]pyrimidin-4(3H)-one scaffolds as mPGES-1 inhibitor are discussed. A set of three analogs were identified with <10 nM potencies in the recombinant human mPGES-1 enzyme and in the A549 cellular assays. These analogs were also found to be potent in the human whole blood assay (<400 nM). Furthermore, the representative compound I was shown to be selective with other prostanoid synthases and was able to effectively regulate PGE2 biosynthesis in clin. relevant inflammatory settings, in comparison with celecoxib. Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Recommanded Product: 2-Amino-4-bromobenzamide.
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Amide – Wikipedia,
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