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

Authors
Hu, LY Ryder, TR Rafferty, MF Cody, WL Lotarski, SM Miljanich, GP Millerman, E Rock, DM Song, YT Stoehr, SJ Taylor, CP Weber, ML Szoke, BG Vartanian, MG
Citation
Ly. Hu et al., N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers, BIOORG MED, 9(6), 1999, pp. 907-912
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
6
Year of publication
1999
Pages
907 - 912
Database
ISI
SICI code
0960-894X(19990322)9:6<907:NANNCC>2.0.ZU;2-Q
Abstract
Selective N-type voltage sensitive calcium channel (VSCC) blockers have sho wn utility in several models of stroke amid pain. We are especially interes ted in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent func tional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, a nd pharmacological evaluation of this series are discussed. (C) 1999 Elsevi er Science Ltd. All rights reserved.