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 › peer-review

25 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

ASJC Scopus subject areas

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

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

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

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.",

author = "Sukumar Sakamuri and Enyedy, {Istvan J.} and Kozikowski, {Alan P.} and Zaman, {Wahiduz A.} and Johnson, {Kenneth M.} and Shaomeng Wang",

note = "Funding Information: The authors are indebted to the National Institute on Drug Abuse (NIDA), National Institutes of Health for their financial support of this work (DA-11545). The lead compound used in the initial screening was provided by the Chemistry Branch, Developmental Therapeutics Program, National Cancer Institute, NIH. ",

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T1 - Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors

AU - Sakamuri, Sukumar

AU - Enyedy, Istvan J.

AU - Kozikowski, Alan P.

AU - Zaman, Wahiduz A.

AU - Johnson, Kenneth M.

AU - Wang, Shaomeng

N1 - Funding Information: The authors are indebted to the National Institute on Drug Abuse (NIDA), National Institutes of Health for their financial support of this work (DA-11545). The lead compound used in the initial screening was provided by the Chemistry Branch, Developmental Therapeutics Program, National Cancer Institute, NIH.

PY - 2001/2/26

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N2 - 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.

AB - 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.

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

Abstract

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