Α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists. Issue 2 (15th January 2016)

• Record Type: Journal Article
• Authors: Verma, Vishal A.; Shore, Daniel G.M.; Chen, Huifen; Chen, Jun; Do, Steven; Hackos, David H.; Kolesnikov, Aleks; Lyssikatos, Joseph P.; Tay, Suzanne; Wang, Lan; Estrada, Anthony A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 2(2016)
• Page Start: 495
• Page End: 498
• Publication Date: 2016-01-15
• Subjects: TRPA1 -- Metabolic stability -- Ion channel; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.11.088
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.