Channelpedia

PubMed 26706172


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: TRP , TRPA , TRPA1



Title: α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.

Authors: Vishal A Verma, Daniel G M Shore, Huifen Chen, Jun Chen, Steven Do, David H Hackos, Aleks Kolesnikov, Joseph P Lyssikatos, Suzanne Tay, Lan Wang, Anthony A Estrada

Journal, date & volume: Bioorg. Med. Chem. Lett., 2016 Jan 15 , 26, 495-8

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/26706172


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.