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
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.