title: Synthesis and structure-activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists.
abstract: Isosteric replacement of the urea group of lead compound 1 led to novel substituted piperidine phenylamide analogues. SAR on the electron-induced effects of various linkers as well as substituents on the phenyl rings and the piperidine nitrogen has been investigated. Many single-digit nanomolar MCH R1 antagonists have been identified from this series.
authors.affiliation: Schering Plough Research Institute, 2015 Galloping Hill Road, MS 2800, Kenilworth, NJ 07033-0539, USA. wen-lian.wu@spcorp.com
authors.forename: Wen-Lian
authors.initials: WL
authors.lastname: Wu
authors.forename: Duane A
authors.initials: DA
authors.lastname: Burnett
authors.forename: Richard
authors.initials: R
authors.lastname: Spring
authors.forename: Li
authors.initials: L
authors.lastname: Qiang
authors.forename: Thavalakulamgara K
authors.initials: TK
authors.lastname: Sasikumar
authors.forename: Martin S
authors.initials: MS
authors.lastname: Domalski
authors.forename: William J
authors.initials: WJ
authors.lastname: Greenlee
authors.forename: Kim
authors.initials: K
authors.lastname: O'Neill
authors.forename: Brian E
authors.initials: BE
authors.lastname: Hawes
mesh_terms: D006801:Humans; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D010880:Piperidines; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor