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

…, JL Mendez-Andino, KM Meyers, N Kim, JA Wos…

Index: Warshakoon, Namal C.; Sheville, Justin; Bhatt, Ritu Tiku; Ji, Wei; Mendez-Andino, Jose L.; Meyers, Kenneth M.; Kim, Nick; Wos, John A.; Mitchell, Chrissy; Paris, Jennifer L.; Pinney, Beth B.; Reizes, Ofer; Hu, X. Eric Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 19 p. 5207 - 5211

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Citation Number: 55

Abstract

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.