Synthesis and SAR of centrally active mGlu(5) positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold

Richard Williams, J.T. Manka, A.L. Rodriguez, P.N. Vinson, C.M. Niswender, C.D. Weaver, C.K. Jones, P.J. Conn, C.W. Lindsley, S.R. Stauffer

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36 Citations (Scopus)

Abstract

This Letter describes the hit-to-lead progression and SAR of a series of biphenyl acetylene compounds derived from an HTS screening campaign targeting the mGlu(5) receptor. 'Molecular switches' were identified that modulated modes of pharmacology, and several compounds within this series were shown to be efficacious in reversal of amphetamine induced hyperlocomotion in rats after ip dosing, a preclinical model that shows similar positive effects with known antipsychotic agents. Published by Elsevier Ltd.
Original languageEnglish
Pages (from-to)1350-1353
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume21
Issue number5
DOIs
Publication statusPublished - 01 Mar 2011

ASJC Scopus subject areas

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

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    Williams, R., Manka, J. T., Rodriguez, A. L., Vinson, P. N., Niswender, C. M., Weaver, C. D., Jones, C. K., Conn, P. J., Lindsley, C. W., & Stauffer, S. R. (2011). Synthesis and SAR of centrally active mGlu(5) positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold. Bioorganic & Medicinal Chemistry Letters, 21(5), 1350-1353. https://doi.org/10.1016/j.bmcl.2011.01.044