title: Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.
abstract: A thorough SAR study of the oxime region of the dual NK(1)/NK(2) antagonist 1 revealed several modifications that result in potent dual antagonists. Follow up SAR studies on a second-generation scaffold demonstrate that certain polar groups on the oxime can improve the dual binding affinity to the subnanomolar range.
authors.affiliation: Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. gregory.reichard@spcorp.com
authors.forename: Gregory A
authors.initials: GA
authors.lastname: Reichard
authors.forename: James
authors.initials: J
authors.lastname: Spitler
authors.forename: Robert
authors.initials: R
authors.lastname: Aslanian
authors.forename: Mwangi wa
authors.initials: Mw
authors.lastname: Mutahi
authors.forename: Neng Yang
authors.initials: NY
authors.lastname: Shih
authors.forename: Ling
authors.initials: L
authors.lastname: Lin
authors.forename: Pauline C
authors.initials: PC
authors.lastname: Ting
authors.forename: John C
authors.initials: JC
authors.lastname: Anthes
authors.forename: John J
authors.initials: JJ
authors.lastname: Piwinski
mesh_terms: D000818:Animals; D019540:Area Under Curve; D006168:Guinea Pigs; D015394:Molecular Structure; D064729:Neurokinin-1 Receptor Antagonists; D010091:Oximes / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D064729:Neurokinin-1 Receptor Antagonists; D010091:Oximes; D018041:Receptors, Neurokinin-2