Abstract:  Melanin concentrating hormone (MCH) is a cyclic 19 amino acid peptide synthesized primarily in the lateral hypothalamus and zona incerta. ICV injection of MCH in rats stimulates food intake while fasting results in an increase in MCH expression. Mice lacking the MCH gene are lean, hypophagic and have increased metabolic rates while mice overexpressing MCH are hyperphagic and overweight. A lean, hypophagic phenotype is also observed in mice in which the MCH receptor (MCHR1) has been deleted. Therefore, it is generally believed that MCHR1 antagonists could be used as a potential treatment for obesity. In this poster, we present the synthesis and SAR of a series of novel thienopyrrolone MCHR1 antagonists, exemplified by 2-(4-chlorophenyl)-5-(4-(2-hydroxy-2-methylpropoxy)-3-methoxyphenyl)-4H-thieno[2,3-c]pyrrol-6(5H)-one (1)  .

Thienopyrrolones as potent melanin-concentrating hormone receptor 1 (MCHR1) antagonists for the treatment of obesity

244th National Meeting (2012)

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