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

Selective N-type Voltage Activated Calcium Channel (VACC) blockers have sho wn utility in several models of stroke and pain. In the process of searchin g for small molecules as N-type calcium channel blockers, we have identifie d a series of N,N-dialkylpeptidylamines (e.g., PD 175069) with potent funct ional activity at N-type VACC. Further modification of the leucine moiety o f PD 175069 with a cyclized ring structure provides a series of novel molec ules. Syntheses and pharmacological evaluation of the series are presented. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.