Synthesis and structure-activity relationships of piperidine-based melanin-concentrating hormone receptor 1 antagonists.
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.
Wu
Wen-Lian
WL
Schering Plough Research Institute, 2015 Galloping Hill Road, MS 2800, Kenilworth, NJ 07033-0539, USA. wen-lian.wu@spcorp.com
Burnett
Duane A
DA
Spring
Richard
R
Qiang
Li
L
Sasikumar
Thavalakulamgara K
TK
Domalski
Martin S
MS
Greenlee
William J
WJ
O'Neill
Kim
K
Hawes
Brian E
BE
D006801:Humans; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D010880:Piperidines; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor