| Literature DB >> 22626552 |
Xenia Beebe1, Daria Darczak, Rodger F Henry, Timothy Vortherms, Richard Janis, Marian Namovic, Diana Donnelly-Roberts, Karen L Kage, Carol Surowy, Ivan Milicic, Wende Niforatos, Andrew Swensen, Kennan C Marsh, Jill M Wetter, Pamela Franklin, Scott Baker, Chengmin Zhong, Gricelda Simler, Erica Gomez, Janel M Boyce-Rustay, Chang Z Zhu, Andrew O Stewart, Michael F Jarvis, Victoria E Scott.
Abstract
A novel 4-aminocyclopentapyrrolidine series of N-type Ca(2+) channel blockers have been discovered. Enantioselective synthesis of the 4-aminocyclopentapyrrolidines was enabled using N-tert-butyl sulfinamide chemistry. SAR studies demonstrate selectivity over L-type Ca(2+) channels. N-type Ca(2+) channel blockade was confirmed using electrophysiological recording techniques. Compound 25 is an N-type Ca(2+) channel blocker that produces antinociception in inflammatory and nociceptive pain models without exhibiting cardiovascular or motor liabilities.Entities:
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Year: 2012 PMID： 22626552 DOI： 10.1016/j.bmc.2012.04.057
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641