On October 5, 2018, Peng, Jingjing; Zhao, Lifen; Wang, Lanlan; Chen, Hui; Qiu, Yunguang; Wang, Jiang; Yang, Huaiyu; Liu, Jun; Liu, Hong published an article.Recommanded Product: 38939-88-7 The title of the article was Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y1 receptor antagonists. And the article contained the following:
A novel series of 2-(phenoxyaryl)-3-urea derivatives I [R1 = H, Me; R2 = n-Bu, 4-F3COC6H4, 5-methoxycarbonyl-2-thienyl, etc.; X = CH, N] were designed, synthesized and biol. evaluated for their anti-thrombotic activity and antiplatelet aggregation study. Most of compounds exhibited good inhibition against P2Y1 receptor among them, compounds I [R1 = H, Me; R2 = 2-methylcyclohexyl, 2-adamantyl, 4-F3COC6H4; X = N] demonstrated good P2Y1 receptor antagonistic potency in vitro (IC50 = 0.62 μM, 0.82 μM, and 0.21 μM, resp.). Four compounds I [R1 = H, Me; R2 = 4-methylcyclohexyl, 4-F3COC6H4, 5-ethoxycarbonyl-2-thienyl, 5-benzyloxycarbonyl-2-thienyl, etc.; X = N] showed good antiplatelet activity. The possible binding modes of compounds with P2Y1 receptor were also explored by mol. docking simulation. The docking studies demonstrated that compound I [R1 = Me; R2 = 4-F3COC6H4; X = N] interacted well with Phe119 through hydrophobic interaction and modestly improved the P2Y1 receptor antagonistic activity. The experimental process involved the reaction of 2-Chloro-4-methyl-1-nitrobenzene(cas: 38939-88-7).Recommanded Product: 38939-88-7
The Article related to phenoxyaryl urea preparation p2y1 antagonist antiplatelet docking sar, 2-(phenoxyaryl)-3-urea derivatives, anti-platelet, p2y(1) receptor antagonist, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Recommanded Product: 38939-88-7
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