α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists

[Display omitted] 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 de...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-01, Vol.26 (2), p.495-498
Hauptverfasser:	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.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Calcium Channels Humans Ion channel Metabolic stability Microsomes, Liver - metabolism Nerve Tissue Proteins - antagonists & inhibitors Pyrrolidines - chemical synthesis Pyrrolidines - pharmacology Rats Stereoisomerism Structure-Activity Relationship Sulfonamides - chemical synthesis Sulfonamides - pharmacology Transient Receptor Potential Channels - antagonists & inhibitors TRPA1 TRPA1 Cation Channel
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Zusammenfassung:	[Display omitted] 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2015.11.088