Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS

A.L. Rodriguez, Y. Zhou, Richard Williams, C.D. Weaver, P.J. Conn, C.W. Lindsley

Research output: Contribution to journalArticle

17 Citations (Scopus)

Abstract

This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold. (C) 2009 Elsevier Ltd. All rights reserved.
Original languageEnglish
Pages (from-to)6502-6506
Number of pages5
JournalBioorganic & Medicinal Chemistry Letters
Volume19
Issue number23
DOIs
Publication statusPublished - 01 Dec 2009

ASJC Scopus subject areas

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

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