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Discovery and SAR of novel tetrahydropyrrolo[3,4-c]pyrazoles as inhibitors of the N-type calcium channel.

Abstract
A novel series of substituted tetrahydropyrrolo[3,4-c]pyrazoles were investigated as blockers of the N-type calcium channel (Cav2.2 channels), a chronic pain target.
AuthorsMichael P Winters, Nalin Subasinghe, Mark Wall, Edward Beck, Michael R Brandt, Michael F A Finley, Yi Liu, Mary Lou Lubin, Michael P Neeper, Ning Qin, Christopher M Flores, Zhihua Sui
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 24 Issue 9 Pg. 2053-6 (May 01 2014) ISSN: 1464-3405 [Electronic] England
PMID24726802 (Publication Type: Journal Article)
CopyrightCopyright © 2014 Elsevier Ltd. All rights reserved.
Chemical References
  • CACNA1B protein, human
  • Calcium Channel Blockers
  • Calcium Channels, N-Type
  • Pyrazoles
Topics
  • Animals
  • Calcium Channel Blockers (chemistry, metabolism, pharmacology)
  • Calcium Channels, N-Type (metabolism)
  • Chronic Pain (drug therapy)
  • Humans
  • Microsomes, Liver (metabolism)
  • Pyrazoles (chemistry, metabolism, pharmacology)
  • Rats
  • Structure-Activity Relationship

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