Melanin Concentrating Hormone (MCH) is a cyclic 19 amino acid peptide predominantly expressed in the CNS. Knock out animal studies suggested that MCH and MCH receptors  (MCHRs) play a role in feeding and energy homeostasis. This presentation describes the design, synthesis, and SAR of a pyrazolopyrrolidinone-derived class of MCHR1 antagonists.  A selective amine analog from this series with a Ki of 1 nM showed significant body weight loss and reduction of food intake in a chronic animal model.

Discovery of pyrazolopyrrolidinone-derived melanin concentrating hormone receptor-1 antagonists as anti-obesity agents

246th National Meeting (2013)

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