Dm. Zimmerman et al., STRUCTURE-ACTIVITY-RELATIONSHIPS OF A SERIES OF 1-SUBSTITUTED-4-METHYLBENZIMIDAZOLE NEUROPEPTIDE Y-1 RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 8(5), 1998, pp. 473-476
The characterization of a novel series of NPY-I receptor antagonists d
erived from the 4-methylbenzimidazole 4 is described. Appropriate subs
titution on the piperidyl nitrogen of 4 led to systematic increases in
Y-1 receptor affinity, to approximately 50-fold, and to the discovery
of the importance of a second basic substituent. (C) 1998 Elsevier Sc
ience Ltd. All rights reserved.