756464-00-3Relevant articles and documents
Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers
Hu, Lain-Yen,Ryder, Todd R.,Nikam, Sham S.,Millerman, Elizabeth,Szoke, Balazs G.,Rafferty, Michael F.
, p. 1121 - 1126 (2007/10/03)
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.