Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: Efficient drug discovery by rational lead hybridization

Jia Zhou, Rong He, Kenneth M. Johnson, Yanping Ye, Alan P. Kozikowski

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

Some piperidine-based nocaine/modafinil hybrid ligands have been designed, synthesized, and found to display an improved potency at all three monoamine transporters and particularly for DAT and/or NET. Some highly active and selective monoamine transporter inhibitors with low nanomolar to subnanomolar potency were identified. Ligands of this type may find important applications as positron emission tomography imaging tools and in the treatment of central nervous system disorders such as depression and sleep apnea.

Original languageEnglish (US)
Pages (from-to)5821-5824
Number of pages4
JournalJournal of Medicinal Chemistry
Volume47
Issue number24
DOIs
StatePublished - Nov 18 2004
Externally publishedYes

Fingerprint

Drug Discovery
Ligands
Positron emission tomography
Central Nervous System Diseases
Sleep Apnea Syndromes
Neurology
Positron-Emission Tomography
Imaging techniques
piperidine
methyl 4-(4-chlorophenyl)-1-methylpiperidine-3-carboxylate
modafinil
Lead
Sleep

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors : Efficient drug discovery by rational lead hybridization. / Zhou, Jia; He, Rong; Johnson, Kenneth M.; Ye, Yanping; Kozikowski, Alan P.

In: Journal of Medicinal Chemistry, Vol. 47, No. 24, 18.11.2004, p. 5821-5824.

Research output: Contribution to journalArticle

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