Author/Authors :
Namal C. Warshakoon، نويسنده , , Justin Sheville، نويسنده , , Ritu Tiku Bhatt، نويسنده , , Wei Ji، نويسنده , , Jose L. Mendez-Andino، نويسنده , , Kenneth M. Meyers، نويسنده , , Nick Kim، نويسنده , , John A. Wos، نويسنده , , Chrissy Mitchell، نويسنده , , Jennifer L. Paris، نويسنده , , Beth B. Pinney، نويسنده , , Ofer Reizes، نويسنده , , X. Eric Hu، نويسنده ,
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.
