Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors

Sukumar Sakamuri, Istvan J. Enyedy, Alan P. Kozikowski, Wahiduz A. Zaman, Kenneth M. Johnson, Shaomeng Wang

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Pharmacophore-based discovery, synthesis, and structure-activity relationship (SAR) of a series of 4-phenyl-1-arylalkyl piperidines are disclosed. These compounds have been evaluated for their ability to inhibit reuptake of dopamine (DA) into striatal nerve endings (synaptosomes). The lead compound 5 and the most potent analogue 43 were found to have significant functional antagonism.

Original languageEnglish (US)
Pages (from-to)495-500
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number4
DOIs
StatePublished - Feb 26 2001

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Piperidines
Lead compounds
Corpus Striatum
Dopamine Plasma Membrane Transport Proteins
Nerve Endings
Synaptosomes
Structure-Activity Relationship
Dopamine
Lead

ASJC Scopus subject areas

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

Cite this

Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. / Sakamuri, Sukumar; Enyedy, Istvan J.; Kozikowski, Alan P.; Zaman, Wahiduz A.; Johnson, Kenneth M.; Wang, Shaomeng.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 4, 26.02.2001, p. 495-500.

Research output: Contribution to journalArticle

Sakamuri, Sukumar ; Enyedy, Istvan J. ; Kozikowski, Alan P. ; Zaman, Wahiduz A. ; Johnson, Kenneth M. ; Wang, Shaomeng. / Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 4. pp. 495-500.
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