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

Autor: Winters MP; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA. Electronic address: mwinter4@its.jnj.com., Subasinghe N; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Wall M; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Beck E; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Brandt MR; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Finley MF; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Liu Y; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Lubin ML; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Neeper MP; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Qin N; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Flores CM; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA., Sui Z; Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 May 01; Vol. 24 (9), pp. 2057-61. Date of Electronic Publication: 2014 Mar 28.
DOI: 10.1016/j.bmcl.2014.03.063
Abstrakt: 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.
(Copyright © 2014 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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