title: Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists.
abstract: A novel series of [6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethyl]-dialkylamines was discovered as potent CRF(1)R antagonists. The optimization of binding affinity in the series by the parallel reaction approach is discussed herein.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA. dmitry.zuev@bms.com
authors.forename: Dmitry
authors.initials: D
authors.lastname: Zuev
authors.forename: Vivekananda M
authors.initials: VM
authors.lastname: Vrudhula
authors.forename: Jodi A
authors.initials: JA
authors.lastname: Michne
authors.forename: Bireshwar
authors.initials: B
authors.lastname: Dasgupta
authors.forename: Sokhom S
authors.initials: SS
authors.lastname: Pin
authors.forename: Xiaohua Stella
authors.initials: XS
authors.lastname: Huang
authors.forename: Dedong
authors.initials: D
authors.lastname: Wu
authors.forename: Qi
authors.initials: Q
authors.lastname: Gao
authors.forename: Jie
authors.initials: J
authors.lastname: Zhang
authors.forename: Matthew T
authors.initials: MT
authors.lastname: Taber
authors.forename: John E
authors.initials: JE
authors.lastname: Macor
authors.forename: Gene M
authors.initials: GM
authors.lastname: Dubowchik
mesh_terms: D006801:Humans; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology; D008744:Methylamines / Q000737:chemistry* / Q000494:pharmacology; D011485:Protein Binding; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000099052:CRF Receptor, Type 1
chemical_list: D007093:Imidazoles; D008744:Methylamines; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1