Title of article :
Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles
Author/Authors :
John J. McAtee، نويسنده , , Jason W. Dodson، نويسنده , , Sarah E. Dowdell، نويسنده , , Karl Erhard، نويسنده , , Gerald R. Girard، نويسنده , , Krista B. Goodman، نويسنده , , Mark A. Hilfiker، نويسنده , , Jian Jin، نويسنده , , Clark A. Sehon، نويسنده , , DeYou Sha، نويسنده , , Dongchuan Shi، نويسنده , , Feng Wang، نويسنده , , Gren Z. Wang، نويسنده , , Ning Wang، نويسنده , , Yonghui Wang، نويسنده , , Andrew Q. Viet، نويسنده , , Catherine C.K. Yuan، نويسنده , , Daohua Zhang ، نويسنده , , Nambi V. Aiyar، نويسنده , , David J. Behm، نويسنده , , et al.، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Pages :
4
From page :
3716
To page :
3719
Abstract :
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 κ-opioid receptor was also explored.
Keywords :
UT , GPR-14 , Antagonist , 7-TM , 7-Transmembrane , Urotensin , HUT , HUT-II
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2008
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
799639
Link To Document :
https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=799639
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