Synthesis and antimycobacterial activity of (+)-usnic acid conjugates.
Daniela CirilloEmanuele BorroniIrene FestosoDiego MontiSergio RomeoDominique MazierLuisella VerottaPublished in: Archiv der Pharmazie (2018)
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.
Keyphrases
- mycobacterium tuberculosis
- multidrug resistant
- escherichia coli
- pulmonary tuberculosis
- healthcare
- public health
- mental health
- working memory
- emergency department
- hiv aids
- high resolution
- drug resistant
- anti inflammatory
- risk assessment
- gram negative
- adverse drug
- cystic fibrosis
- climate change
- health information
- health promotion