Synthesis and SAR of selective small molecule neuropeptide Y Y2 receptor antagonists

  • Bioorg Med Chem Lett. 2012 Jun 15;22(12):3916-20. doi: 10.1016/j.bmcl.2012.04.107.
Gopi Kumar Mittapalli  1 ,  Danielle Vellucci ,  Jun Yang ,  Marion Toussaint ,  Shaun P Brothers ,  Claes Wahlestedt ,  Edward Roberts
Affiliations
  • 1. Department of Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines Rd, La Jolla, CA 92037, USA.
PMID: 22607676 DOI: 10.1016/j.bmcl.2012.04.107
Abstract

Highly potent and selective small molecule neuropeptide Y Y2 receptor antagonists are reported. The systematic SAR exploration of a hit molecule N-(4-ethoxyphenyl)-4-[hydroxy(diphenyl)methyl]piperidine-1-carbothioamide, identified from HTS, led to the discovery of highly potent NPY Y2 antagonists 16 (CYM 9484) and 54 (CYM 9552) with IC(50) values of 19 nM and 12 nM respectively.

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