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.

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