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Molecules 2018, 23(7), 1753; https://doi.org/10.3390/molecules23071753

Synthesis and Biological Activity of Sterol 14α-Demethylase and Sterol C24-Methyltransferase Inhibitors

Department of Biology, Geology and Physical Sciences, Sul Ross State University, Alpine, TX 79832, USA
Academic Editors: Wenxu Zhou and De-an Guo
Received: 20 June 2018 / Revised: 13 July 2018 / Accepted: 15 July 2018 / Published: 17 July 2018

Abstract

Sterol 14α-demethylase (SDM) is essential for sterol biosynthesis and is the primary molecular target for clinical and agricultural antifungals. SDM has been demonstrated to be a valid drug target for antiprotozoal therapies, and much research has been focused on using SDM inhibitors to treat neglected tropical diseases such as human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis. Sterol C24-methyltransferase (24-SMT) introduces the C24-methyl group of ergosterol and is an enzyme found in pathogenic fungi and protozoa but is absent from animals. This difference in sterol metabolism has the potential to be exploited in the development of selective drugs that specifically target 24-SMT of invasive fungi or protozoa without adversely affecting the human or animal host. The synthesis and biological activity of SDM and 24-SMT inhibitors are reviewed herein. View Full-Text
Keywords: sterol biosynthesis; sterol 14α-demethylase; sterol C24-methyltransferase; mechanism-based inactivators; antifungals; azoles; antiparasitic drugs; human African trypanosomiasis; Chagas disease; synthesis sterol biosynthesis; sterol 14α-demethylase; sterol C24-methyltransferase; mechanism-based inactivators; antifungals; azoles; antiparasitic drugs; human African trypanosomiasis; Chagas disease; synthesis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Leaver, D.J. Synthesis and Biological Activity of Sterol 14α-Demethylase and Sterol C24-Methyltransferase Inhibitors. Molecules 2018, 23, 1753.

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