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

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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-05, Vol.24 (9), p.2053-2056
Main Authors: Winters, Michael P., Subasinghe, Nalin, Wall, Mark, Beck, Edward, Brandt, Michael R., Finley, Michael F.A., Liu, Yi, Lubin, Mary Lou, Neeper, Michael P., Qin, Ning, Flores, Christopher M., Sui, Zhihua
Format: Article
Language:English
Subjects:
Animals
Calcium Channel Blockers - chemistry
Calcium Channel Blockers - metabolism
Calcium Channel Blockers - pharmacology
Calcium Channels, N-Type - metabolism
Cav2.2 blockers
Chronic Pain - drug therapy
Humans
Microsomes, Liver - metabolism
N-type calcium channel
Pain
Pyrazoles - chemistry
Pyrazoles - metabolism
Pyrazoles - pharmacology
Rats
Structure-Activity Relationship
Tetrahydropyrrolo[3,4-c]pyrazoles
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.03.062