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

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

  • Bioorg Med Chem Lett. 2010 Apr 1;20(7):2106-10. doi: 10.1016/j.bmcl.2010.02.058.
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,  Nancy N Tsou,  Richard G Ball,  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 Jr,  Ravi P Nargund
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. shuwen_he@merck.com
PMID: 20207541 DOI: 10.1016/j.bmcl.2010.02.058
Abstract

We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.

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