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The Chemistry and Pharmacology of Tetrahydropyridines

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Tetrahydropyridine (THP) moiety is a part of many biologically active systems. The discovery of the neurotoxic properties of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) as well as numerous alkaloids, prompted extensive research on the synthesis and pharmacological properties of these compounds. The goal was extending the database for structure-activity relationship (SAR) studies. Consequently, many promising drug candidates were designed and a lot more are under clinical study. The current paper reviews the most popular approaches for the synthesis of THP derivatives. The pharmacological characteristics of some THP derivatives are summarized together with composite of the data from their in vitro, ex vivo and in vivo assays.
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Keywords: pharmacology; structure-activity relationship; synthesis; tetrahydropyridines

Document Type: Review Article

Affiliations: College of Pharmacy and Pharmaceutical Sciences, Florida A University, Tallahassee, FL 32307, USA.

Publication date: 2005-03-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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