N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers

  • Bioorg Med Chem Lett. 1999 Mar 22;9(6):907-12. doi: 10.1016/s0960-894x(99)00100-6.
L Y Hu  1 ,  T R Ryder ,  M F Rafferty ,  W L Cody ,  S M Lotarski ,  G P Miljanich ,  E Millerman ,  D M Rock ,  Y Song ,  S J Stoehr ,  C P Taylor ,  M L Weber ,  B G Szoke ,  M G Vartanian
Affiliations
  • 1. Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
PMID: 10206559 DOI: 10.1016/s0960-894x(99)00100-6
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.

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