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N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers
L Y Hu1, T R Ryder, M F Rafferty
1Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Bioorganic & Medicinal Chemistry Letters
|April 17, 1999
Abstract:
Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown utility in several models of stroke and pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed.