Discovery and SAR of a novel series of 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles as N-type calcium channel inhibitors.

Research paper by Michael P MP Winters, Nalin N Subasinghe, Mark M Wall, Edward E Beck, Michael R MR Brandt, Michael F A MF Finley, Yi Y Liu, Mary Lou ML Lubin, Michael P MP Neeper, Ning N Qin, Christopher M CM Flores, Zhihua Z Sui

Indexed on: 15 Apr '14Published on: 15 Apr '14Published in: Bioorganic & Medicinal Chemistry Letters


A novel series of substituted 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles were investigated as N-type calcium channel blockers (Cav2.2 channels), a chronic pain target. One compound was active in vivo in the rat CFA pain model.