Discovery and optimization of a novel Neuromedin B receptor antagonist.
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.
Fu
Jiasheng
J
Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. jfu@amgen.com
Shuttleworth
Stephen J
SJ
Connors
Richard V
RV
Chai
Anne
A
Coward
Peter
P
D000818:Animals; D001570:Benzodiazepinones / Q000138:chemical synthesis* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004583:Electrons; D019886:Gastrin-Releasing Peptide / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D008956:Models, Chemical; D010455:Peptides / Q000737:chemistry; D018004:Receptors, Bombesin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D001570:Benzodiazepinones; D008024:Ligands; D010455:Peptides; D018004:Receptors, Bombesin; D019886:Gastrin-Releasing Peptide