Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.
Bioorganic & Medicinal Chemistry Letters(2008)
摘要
Redesign of the potent human urotensin-II antagonist 1 with the 2-pyrrolidinylmethyl-3-phenyl-piperidine core to a new chemical series with a substituted N-methyl-2-(1-pyrrolidinyl)ethanamine core as in 17 resulted in compounds with improved PK profiles.
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关键词
Urotensin,HUT,HUT-II,UT,GPR-14,Antagonist,7-TM,7-Transmembrane
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