Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers.
Basic Information
ID: ALA1131677
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers.
Authors: Hu LY, Ryder TR, Nikam SS, Millerman E, Szoke BG, Rafferty MF.
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.
CiteXplore: 10328297
DOI: 10.1016/s0960-894x(99)00160-2
Patent ID: ┄