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

11 Citations (Scopus)

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

Fingerprint

Mazindol
Thiazoles
Dopamine Plasma Membrane Transport Proteins
Dopamine
diphenyl

ASJC Scopus subject areas

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

Cite this

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

In: Bioorganic and Medicinal Chemistry Letters, Vol. 12, No. 13, 08.07.2002, p. 1775-1778.

Research output: Contribution to journalArticle

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