title: Synthesis and evaluation of 2-anilino-3-phenylsulfonyl-6-methylpyridines as corticotropin-releasing factor1 receptor ligands.
abstract: A novel series of 2-anilino-3-phenylsulfonyl-6-methylpyridines was synthesized and evaluated as corticotropin-releasing factor receptor ligands. Structure-activity relationship studies focused primarily on optimization of the 3-phenylsulfonyl group. Compounds within this series were identified which showed potent binding affinity for the CRF1 receptor. Selected compounds were examined in a rat pharmacokinetic study and were found to have oral bioavailabilities ranging from 16 to 35%.
authors.affiliation: Discovery Chemistry, Bristol-Myers Squibb Company, Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. richard.hartz@bms.com
authors.forename: Richard A
authors.initials: RA
authors.lastname: Hartz
authors.forename: Argyrios G
authors.initials: AG
authors.lastname: Arvanitis
authors.forename: Charles
authors.initials: C
authors.lastname: Arnold
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Rescinito
authors.forename: Kimberly L
authors.initials: KL
authors.lastname: Hung
authors.forename: Ge
authors.initials: G
authors.lastname: Zhang
authors.forename: Harvey
authors.initials: H
authors.lastname: Wong
authors.forename: David R
authors.initials: DR
authors.lastname: Langley
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Gilligan
authors.forename: George L
authors.initials: GL
authors.lastname: Trainor
mesh_terms: D000284:Administration, Oral; D000818:Animals; D018360:Crystallography, X-Ray; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D011725:Pyridines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D000099052:CRF Receptor, Type 1
chemical_list: D008024:Ligands; D011725:Pyridines; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1