212691-73-1Relevant articles and documents
Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y1 receptor antagonists
Peng, Jingjing,Zhao, Lifen,Wang, Lanlan,Chen, Hui,Qiu, Yunguang,Wang, Jiang,Yang, Huaiyu,Liu, Jun,Liu, Hong
, p. 302 - 310 (2018/09/18)
A novel series of 2-(phenoxyaryl)-3-urea derivatives were designed, synthesized, and biologically evaluated for their anti-thrombotic activity. Most of compounds exhibited good inhibition against P2Y1 receptor. Among them, three compounds 11, 12, and 13 demonstrated good P2Y1 receptor antagonistic potency in vitro (IC50 = 0.62 μM, 0.82 μM, and 0.21 μM, respectively). In antiplatelet aggregation study, four compounds 2, 3, 9, and 13 showed good antiplatelet activity. The possible binding modes of compounds with P2Y1 receptor were also explored by molecular docking simulation. The docking studies demonstrated that compound 13 interacted well with Phe119 through hydrophobic interaction and modestly improved the P2Y1 receptor antagonistic activity, making it justifiable for further investigation.
AMINO-BENZAZOLES AS P2Y1 RECEPTOR INHIBITORS
-
Page/Page column 106, (2008/06/13)
The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating dis
Arylmethanesulfonates are convenient latent phenols in the nucleophilic aromatic substitution reaction
Dinsmore, Christopher J.,Zartman, C. Blair
, p. 3989 - 3990 (2007/10/03)
The methanesulfonyl protecting group for a phenol is conveniently unmasked under the conditions of the S(N)Ar reaction with an activated aryl halide, producing diarylether products directly. The method is advantageous when the preparation of a phenol substrate requires O-protection, since the selection of the robust methanesulfonate as a latent phenol obviates a deprotection step prior to the S(N)Ar reaction.