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

doi:10.1016/S0960-894X(00)00703-4

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

Pharmacology & Toxicology

Research output: Contribution to journal › Article

22 Scopus citations

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 language	English (US)
Pages (from-to)	495-500
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	4
DOIs	https://doi.org/10.1016/S0960-894X(00)00703-4
State	Published - Feb 26 2001

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ASJC Scopus subject areas

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

Cite this

Sakamuri, S., Enyedy, I. J., Kozikowski, A. P., Zaman, W. A., Johnson, K. M., & Wang, S. (2001). Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors. Bioorganic and Medicinal Chemistry Letters, 11(4), 495-500. https://doi.org/10.1016/S0960-894X(00)00703-4

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 journal › Article

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10.1016/S0960-894X(00)00703-4