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Synthesis and antimycobacterial activity of (+)‐usnic acid conjugates
Author(s) -
Cirillo Daniela,
Borroni Emanuele,
Festoso Irene,
Monti Diego,
Romeo Sergio,
Mazier Dominique,
Verotta Luisella
Publication year - 2018
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201800177
Subject(s) - usnic acid , antimycobacterial , tuberculosis , mycobacterium tuberculosis , microbiology and biotechnology , mycobacterium , chemistry , ethambutol , pharmacology , biology , lichen , medicine , botany , pathology
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.