Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers

  • Bioorg Med Chem Lett. 1999 Apr 19;9(8):1121-6. doi: 10.1016/s0960-894x(99)00160-2.
L Y Hu  1 ,  T R Ryder ,  S S Nikam ,  E Millerman ,  B G Szoke ,  M F Rafferty
Affiliations
  • 1. Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
PMID: 10328297 DOI: 10.1016/s0960-894x(99)00160-2
Abstract

Selective N-type Voltage Activated Calcium Channel (VACC) blockers have shown utility in several models of stroke and pain. In the process of searching for small molecules as N-type calcium channel blockers, we have identified a series of N,N-dialkylpeptidylamines (e.g., PD 175069) with potent functional activity at N-type VACC. Further modification of the leucine moiety of PD 175069 with a cyclized ring structure provides a series of novel molecules. Syntheses and pharmacological evaluation of the series are presented.

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