Antituberculosis activity of alkylated mulinane diterpenoids
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Published on: October 25, 2024
Gloria María Molina-Salinas1, Jorge Bórquez, Salvador Said-Fernández
1Grupo de Química Orgánica, Unidad de Biotecnología del Centro de Investigación Científica de Yucatán, Calle 43 No 130, Colonia Chuburná, Mérida, Yucatán, 97200 México. gmolina70@gmail.com
Abstract:
Natural azorellane and mulinane diterpenoids show antituberculosis activity, which is increased by methylation of their free carboxyl group. We have systematically investigated the effect of alkylation in this class of diterpenoids and found that the profile of bioactivity is relatively unaffected by the introduction of short alkyl groups, both linear and branched. In this investigation, three semisynthetic diterpenoids, 13 hydroxy-mulin-11-en-20-oic acid n-propyl ester (3) and the n-propyl (19) and n-butyl (20) esters of isomulinic acid, showed the strongest antituberculosis activity (MIC=6.25 microg/mL) against a drug-resistant strain of Mycobacterium tuberculosis.
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