| Literature DB >> 26706172 |
Vishal A Verma1, Daniel G M Shore1, Huifen Chen1, Jun Chen1, Steven Do1, David H Hackos1, Aleks Kolesnikov1, Joseph P Lyssikatos1, Suzanne Tay1, Lan Wang1, Anthony A Estrada1.
Abstract
A series of α-aryl pyrrolidine sulfonamide TRPA1 antagonists were advanced from an HTS hit to compounds that were stable in liver microsomes with retention of TRPA1 potency. Metabolite identification studies and physicochemical properties were utilized as a strategy for compound design. These compounds serve as starting points for further compound optimization.Entities:
Keywords: Ion channel; Metabolic stability; TRPA1
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Year: 2015 PMID： 26706172 DOI： 10.1016/j.bmcl.2015.11.088
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823