2. Academic Validation
  3. Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity

Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity

  • Bioorg Med Chem Lett. 2010 Aug 1;20(15):4399-405. doi: 10.1016/j.bmcl.2010.06.062.
Shuwen He 1,  Zhixiong Ye,  Peter H Dobbelaar,  Iyassu K Sebhat,  Liangqin Guo,  Jian Liu,  Tianying Jian,  Yingjie Lai,  Christopher L Franklin,  Raman K Bakshi,  James P Dellureficio,  Qingmei Hong,  David H Weinberg,  Tanya Macneil,  Rui Tang,  Alison M Strack,  Constantin Tamvakopoulos,  Qianping Peng,  Randy R Miller,  Ralph A Stearns,  Howard Y Chen,  Airu S Chen,  Tung M Fong,  Matthew J Wyvratt Jr,  Ravi P Nargund
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. shuwen_he@merck.com
PMID: 20598882 DOI: 10.1016/j.bmcl.2010.06.062
Abstract

We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds can afford high potency on MC4R as well as good rodent pharmacokinetic profiles. Compound 1r (MK-0489) demonstrates MC4R mediated reduction of food intake and body weight in mouse models. Compound 1r is efficacious in 14-day diet-induced obese (DIO) rat models.

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