Peng, Jingjing published the artcileDesign, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y1 receptor antagonists, Application of 2-Morpholinoethanol, the publication is European Journal of Medicinal Chemistry (2018), 302-310, database is CAplus and MEDLINE.
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.
European Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Application of 2-Morpholinoethanol.
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