PubMed |
Abstract |
RScore(About this table) |
18550370 |
Qiao JX, Cheney DL, Alexander RS, Smallwood AM, King SR, He K, Rendina AR, Luettgen JM, Knabb RM, Wexler RR, Lam PY: Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4118-23. Epub 2008 May 29.
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82(1,1,1,2) |
Details |
19721266 |
Jia ZJ, Scarborough RM, Zhang P, Halfon S, Arfsten AE, Sinha U, Zhu BY: Design, synthesis and discovery of 1-(2-(6-Chloro-3-methylsulfonyl)-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent factor Xa inhibitors. Chem Pharm Bull. 2009 Sep;57(9):1004-7.
Based upon the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides reported in our previous communications, we designed and discovered 2-(6-chloro-3-methylsulfonyl)-naphthyl as an optimal factor Xa S1 binding element. |
63(0,2,2,3) |
Details |
19193009 |
de Candia M, Liantonio F, Carotti A, De Cristofaro R, Altomare C: Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation. J Med Chem. 2009 Feb 26;52(4):1018-28.
Two congeners of N-{[3-(1,1'-biphenyl-4-yl) methoxy] phenyl}piperidine-4-carboxamide (7m and 7p) proved to be potent FXa-selective inhibitors (K (i) = 130 and 57 nM, respectively) and antiplatelet agents and were identified as leads for developing new dual function antithrombotic drugs. |
2(0,0,0,2) |
Details |