32266-56-1Relevant articles and documents
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists
Giordanetto, Fabrizio,Karlsson, Olle,Lindberg, Jan,Larsson, Lars-Olof,Linusson, Anna,Evertsson, Emma,Morgan, David G.A.,Inghardt, Tord
, p. 4232 - 4241 (2008/12/21)
We herein report the optimization of cyclopentane- and cyclohexane-1,3-diamine derivatives as novel and potent MCH-R1 antagonists. Structural modifications of the 2-amino-quinoline and thiophene moieties found in the initial lead compound served to improve its metabolic stability profile and MCH-R1 affinity, and revealed unprecedented SAR when compared to other 2-amino-quinoline-containing MCH-R1 antagonists.