Abstract
The biotransformations of artemisinin and artemisinin derivatives leading to metabolites that may serve as prospective candidates for antimalarial evaluation or as starting materials for hemisynthesis of antimalarial derivatives are reviewed, focusing on the preparation of regio- and stereoselectively hydroxylated derivatives still possessing the 1,2,4- trioxane structure that can be used as scaffolds for the production of novel antimalarials with increased water solubility, lower toxicity and decreased potential for resistance. A special emphasis has been also placed on the recent manufacturing of artemisinin and derivatives via microbiological methods, involving cloning and overexpression of biosynthetic enzymes and allowing to design an alternative route for artemisinin production.
Keywords: Arteether, artemether, artesunate, artemisia annua, bacteria, fungi, hydroxylations, synthetic reactions, molecular diversity, microbial generation.
Current Bioactive Compounds
Title:Microbial Transformations of Artemisinin and Artemisinin Derivatives: an Example of the Microbial Generation of Molecular Diversity
Volume: 8 Issue: 2
Author(s): Robert Azerad
Affiliation:
Keywords: Arteether, artemether, artesunate, artemisia annua, bacteria, fungi, hydroxylations, synthetic reactions, molecular diversity, microbial generation.
Abstract: The biotransformations of artemisinin and artemisinin derivatives leading to metabolites that may serve as prospective candidates for antimalarial evaluation or as starting materials for hemisynthesis of antimalarial derivatives are reviewed, focusing on the preparation of regio- and stereoselectively hydroxylated derivatives still possessing the 1,2,4- trioxane structure that can be used as scaffolds for the production of novel antimalarials with increased water solubility, lower toxicity and decreased potential for resistance. A special emphasis has been also placed on the recent manufacturing of artemisinin and derivatives via microbiological methods, involving cloning and overexpression of biosynthetic enzymes and allowing to design an alternative route for artemisinin production.
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Cite this article as:
Azerad Robert, Microbial Transformations of Artemisinin and Artemisinin Derivatives: an Example of the Microbial Generation of Molecular Diversity, Current Bioactive Compounds 2012; 8 (2) . https://dx.doi.org/10.2174/157340712801784750
DOI https://dx.doi.org/10.2174/157340712801784750 |
Print ISSN 1573-4072 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6646 |
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