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Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain

Xenia Beebe, Clinton M. Yeung,Daria Darczak,Shashank Shekhar,Timothy A. Vortherms,Loan Miller,Ivan Milicic,Andrew M. Swensen,Chang Z. Zhu,Patricia Banfor,Jill M. Wetter,Kennan C. Marsh, Michael F. Jarvis,Victoria E. Scott,Michael R. Schrimpf,Chih-Hung Lee

Bioorganic & Medicinal Chemistry Letters（2013）

Cited 8|Views9
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Abstract
A novel series of N-type calcium channel inhibitors have been discovered. Optimization of potency and HT-ADME properties provides 4-aminocyclopentapyrrolidines with analgesic efficacy after oral dosing.
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Key words
N-type calcium channels,SAR,Enantiomeric synthesis,Microsomal stability,Analgesia
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