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
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. [email protected]
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.