This article describes the microbial conversion of the plant-derived antimalarial drug, artemisinin to 7β-hydroxyartemisinin, 4α-hydroxy-1-deoxoartemisinin, 6β-hydroxyartemisinin and 5β-hydroxyartemisinin, and the conversion of 10-deoxoartemisinin to 5β-hydroxy-10-deoxoartemisinin, 4α-hydroxy-1,10-d...
This article describes the microbial conversion of the plant-derived antimalarial drug, artemisinin to 7β-hydroxyartemisinin, 4α-hydroxy-1-deoxoartemisinin, 6β-hydroxyartemisinin and 5β-hydroxyartemisinin, and the conversion of 10-deoxoartemisinin to 5β-hydroxy-10-deoxoartemisinin, 4α-hydroxy-1,10-dideoxoartemisinin, 7β-hydroxy-10-deoxoartemisinin, and 15-hydroxy-10-deoxoartemisinin. Each of these structural hydroxy metabolite variants was produced in quantities suitable for derivatization to produce hundreds of novel substituted derivatives via parallel and combinatorial syntheses. The obtained metabolites were produced through bioconversion by Aspergillus niger, Cunninghamella elegans, Eurotium amstelodami, and Mucor rammanianus.
ISBN 1-9336990-7-8 Editors: Singh, V.K.;Govil, J.N.;Arunachalam, C. Phytochemistry and pharmacology III 2007 pp. 115-138