Quinazoline and benzimidazole MCH-1R antagonists

Rosa Arienzo; Sue Cramp; Hazel J Dyke; Peter M Lockey; Dennis Norman; Alan G Roach; Phil Smith; Melanie Wong; Stephen P Wren

doi:10.1016/j.bmcl.2006.11.092

Quinazoline and benzimidazole MCH-1R antagonists

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1403-7. doi: 10.1016/j.bmcl.2006.11.092. Epub 2006 Dec 2.

Authors

Rosa Arienzo¹, Sue Cramp, Hazel J Dyke, Peter M Lockey, Dennis Norman, Alan G Roach, Phil Smith, Melanie Wong, Stephen P Wren

Affiliation

¹ Argenta Discovery Limited, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, UK.

PMID: 17178222
DOI: 10.1016/j.bmcl.2006.11.092

Abstract

We have modified the previously reported 2-aminoquinoline 1 to provide two novel series of MCH-1R antagonists. Representative compounds from the quinazoline and benzimidazole series have been shown to be potent and selective, with promising in vitro eADME profiles.

MeSH terms

Benzimidazoles / chemical synthesis*
Benzimidazoles / pharmacology
Humans
Inhibitory Concentration 50
Protein Binding
Quinazolines / chemical synthesis*
Quinazolines / pharmacology
Receptors, Somatostatin / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Benzimidazoles
MCHR1 protein, human
Quinazolines
Receptors, Somatostatin
benzimidazole