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Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles

作者	McAtee, JJ; Dodson, JW; Dowdell, SE; Erhard, K; Girard, GR; Goodman, KB; Hil, MA; Jin, J; Sehon, CA; Sha, DY; Shi, DC; Wang, F; Wang, GZ; Wang, N; Wang, YH; Viet, AQ; Yuan, CCK; Zhang, DH; Aiyar, NV; Behm, DJ; Carballo, LH; Evans, CA; Fries, HE; Nagilla, R; Roethke, TJ; Xu, XP; Douglas, SA; Neeb, MJ

选自	期刊 Bioorganic & Medicinal Chemistry Letters; 卷期 2008年18-13; 页码 3716-3719

关联知识点

[摘要]：Lead compound 1 was successfully redesigned to provide compounds with improved pharmacokinetic profiles for this series of human urotensin-II antagonists. Replacement of the 2-pyrrolidinylmethyl-3-phenyl-piperidine core of 1 with a substituted N-methyl-2-(1-pyrrolidinyl) ethanamine core as in compound 7 resulted in compounds with improved oral bioavailability in rats. The relationship between stereochemistry and selectivity for hUT over the kappa-opioid receptor was also explored. (C) 2008 Elsevier Ltd. All rights reserved.
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