| Literature DB >> 18722118 |
Markian M Stec1, Yunxin Bo, Partha P Chakrabarti, Lillian Liao, Mqhele Ncube, Nuria Tamayo, Rami Tamir, Narender R Gavva, James J S Treanor, Mark H Norman.
Abstract
Clinical candidate AMG 517 (1) is a potent antagonist toward multiple modes of activation of TRPV1; however, it suffers from poor solubility. Analogs with various substituents at the R region of 3 were prepared to improve the solubility while maintaining the potent TRPV1 activity of 1. Compounds were identified that maintained potency, had good pharmacokinetic properties, and improved solubility relative to 1.Entities:
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Year: 2008 PMID： 18722118 DOI： 10.1016/j.bmcl.2008.07.112
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823