Discovery of substituted 3,4-Diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol

Istvan J. Enyedy, Jiansuo Wang, Wahiduz A. Zaman, Kenneth M. Johnson, Shaomeng Wang

Research output: Contribution to journalArticle

12 Scopus citations

Abstract

Substituted 3,4-diphenyl-1,3-thiazols were identified as a class of novel and potent monoamine transporter inhibitors through a 3-D pharmacophore search using a new pharmacophore model derived from mazindol. The most potent compound (13) has Ki values of 24 and 23 nM in binding to dopamine transporter and inhibition of dopamine reuptake, respectively.

Original languageEnglish (US)
Pages (from-to)1775-1778
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number13
DOIs
StatePublished - Jul 8 2002

ASJC Scopus subject areas

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

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