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

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

Affiliation

  • 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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