title: Synthesis and SAR of 1,3-disubstituted cyclohexylmethyl urea and amide derivatives as non-peptidic motilin receptor antagonists.
abstract: A series of 1,3-disubstituted cyclohexylmethyl urea and amide derivatives were synthesized as motilin receptor antagonists. Starting from known motilin antagonists, 1a and 1b, the cyclopentene scaffold was replaced and the four recognition elements optimized to arrive at a potent novel series.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 1000 Rt. 202, PO Box 300, Raritan, NJ 08869, USA. sgjcej@juno.com
authors.forename: Sigmond G
authors.initials: SG
authors.lastname: Johnson
authors.forename: Joseph W
authors.initials: JW
authors.lastname: Gunnet
authors.forename: John B
authors.initials: JB
authors.lastname: Moore
authors.forename: William
authors.initials: W
authors.lastname: Miller
authors.forename: Pam
authors.initials: P
authors.lastname: Wines
authors.forename: Ralph A
authors.initials: RA
authors.lastname: Rivero
authors.forename: Don
authors.initials: D
authors.lastname: Combs
authors.forename: Keith T
authors.initials: KT
authors.lastname: Demarest
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D003510:Cyclohexanes / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D015394:Molecular Structure; D011964:Receptors, Gastrointestinal Hormone / Q000037:antagonists & inhibitors*; D018013:Receptors, Neuropeptide / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014508:Urea / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000577:Amides; D003510:Cyclohexanes; D011964:Receptors, Gastrointestinal Hormone; D018013:Receptors, Neuropeptide; C050802:motilin receptor; D014508:Urea