Discovery and optimization of a novel Neuromedin B receptor antagonist

Jiasheng Fu; Stephen J Shuttleworth; Richard V Connors; Anne Chai; Peter Coward

doi:10.1016/j.bmcl.2009.05.124

Discovery and optimization of a novel Neuromedin B receptor antagonist

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4264-7. doi: 10.1016/j.bmcl.2009.05.124. Epub 2009 Jun 6.

Authors

Jiasheng Fu¹, Stephen J Shuttleworth, Richard V Connors, Anne Chai, Peter Coward

Affiliation

¹ Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. jfu@amgen.com

PMID: 19553112
DOI: 10.1016/j.bmcl.2009.05.124

Abstract

The discovery and parallel synthesis of potent, small molecule antagonists of Neuromedin B receptor based on the ary-hexahydro-dibenzodiazepin-1-one core is described.

MeSH terms

Animals
Benzodiazepinones / chemical synthesis*
Benzodiazepinones / pharmacology
Chemistry, Pharmaceutical / methods*
Dose-Response Relationship, Drug
Drug Design
Electrons
Gastrin-Releasing Peptide / chemistry
HeLa Cells
Humans
Inhibitory Concentration 50
Ligands
Models, Chemical
Peptides / chemistry
Receptors, Bombesin / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Benzodiazepinones
Ligands
Peptides
Receptors, Bombesin
Gastrin-Releasing Peptide