BIOACTIVE CONFORMATIONS OF LIGANDS FOR THE CALCIUM-CHANNEL ALPHA(2)DELTA GABAPENTIN BINDING-SITE

Citation
Js. Bryans et al., BIOACTIVE CONFORMATIONS OF LIGANDS FOR THE CALCIUM-CHANNEL ALPHA(2)DELTA GABAPENTIN BINDING-SITE, Medicinal chemistry research, 8(3), 1998, pp. 153-162
Citations number
5
Categorie Soggetti
Chemistry Medicinal
ISSN journal
10542523
Volume
8
Issue
3
Year of publication
1998
Pages
153 - 162
Database
ISI
SICI code
1054-2523(1998)8:3<153:BCOLFT>2.0.ZU;2-0
Abstract
Conformational search and comparison of 3 series of ligands for the ca lcium channel alpha(2)delta gabapentin binding site have been used to further define the bioactive conformation of gabapentin. This analysis explains the stereoselectivities of the ligands and has led to the sy nthesis of a high affinity alkylated gabapentin analogue.