Design and synthesis of substituted quinolines as novel and selective melanin concentrating hormone antagonists as anti-obesity agents

A novel series of substituted quinoline analogs were designed and synthesized as potent and selective melanin concentrating hormone (MCH) antagonists. These analogs show potent (nM) activity ( 12a– k) with a moderate selectivity. Conversely, the conformationally constrained thienopyrimidinone analogs ( 18a– g) showed improved activity in MCH-1R and selectivity over 5HT2C.