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

Gopi Kumar Mittapalli, Danielle Vellucci, Jun Yang, Marion Toussaint, Shaun P. Brothers, Claes Wahlestedt, Edward Roberts

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

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 IC50 values of 19 nM and 12 nM respectively.

Original languageEnglish (US)
Pages (from-to)3916-3920
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume22
Issue number12
DOIs
StatePublished - Jun 15 2012
Externally publishedYes

Keywords

  • Antagonist
  • Carbamate
  • Neuropeptide Y Y2
  • Structure-activity relationship
  • Thiourea

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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