Synthesis and antimycobacterial activity of (+)-usnic acid conjugates

D Cirillo, E Borroni, I Festoso, D Monti, S Romeo, D Mazier, L Verotta

Research output: Contribution to journalArticle

Abstract

New therapeutics are urgently needed to fight tuberculosis and mycobacteria-related diseases that are a major health hazard especially in poor countries. Natural products have been the source of important antitubercular drugs in the past and still need to receive attention as a potent reservoir of chemical structures. Fifteen known and two new (+)-usnic acid (a benzofurandione formerly isolated from lichens) enamines and hydrazones are here described and tested against sensitive and multidrug-resistant strains of mycobacteria. Among several (+)-usnic acid conjugates, PS14 and PS18 showed potent activity against both susceptible and resistant Mycobacterium tuberculosis strains (MIC values of 1–32 and 2–32 mg/L, respectively) comparable with MIC of other antitubercular drugs already in use for tuberculosis treatment. © 2018 Deutsche Pharmazeutische Gesellschaft
Original languageEnglish
Article numbere1800177
JournalArchiv der Pharmazie
Volume351
DOIs
Publication statusPublished - 2018

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    Cirillo, D., Borroni, E., Festoso, I., Monti, D., Romeo, S., Mazier, D., & Verotta, L. (2018). Synthesis and antimycobacterial activity of (+)-usnic acid conjugates. Archiv der Pharmazie, 351, [e1800177]. https://doi.org/10.1002/ardp.201800177