Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist

  • Bioorg Med Chem Lett. 2011 Apr 15;21(8):2330-4. doi: 10.1016/j.bmcl.2011.02.090.
Qingmei Hong  1 ,  Raman K Bakshi ,  Brenda L Palucki ,  Min K Park ,  Zhixiong Ye ,  Shuwen He ,  Patrick G Pollard ,  Iyassu K Sebhat ,  Jian Liu ,  Liangqin Guo ,  Doreen E Cashen ,  William J Martin ,  David H Weinberg ,  Tanya MacNeil ,  Rui Tang ,  Constantin Tamvakopoulos ,  Qianping Peng ,  Randy R Miller ,  Ralph A Stearns ,  Howard Y Chen ,  Airu S Chen ,  Alison M Strack ,  Tung M Fong ,  D Euan MacIntyre ,  Matthew J Wyvratt ,  Ravi P Nargund
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. [email protected]
PMID: 21439820 DOI: 10.1016/j.bmcl.2011.02.090
Abstract

We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.

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