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.
Synthesis and antimycobacterial activity of (+)-usnic acid conjugates / D. Cirillo, E. Borroni, I. Festoso, D. Monti, S. Romeo, D. Mazier, L. Verotta. - In: ARCHIV DER PHARMAZIE. - ISSN 0365-6233. - 351:12(2018 Dec), pp. e1800177.1-e1800177.9.
Titolo: | Synthesis and antimycobacterial activity of (+)-usnic acid conjugates |
Autori: | BORRONI, EMANUELE (Secondo) VEROTTA, LUISELLA (Ultimo) (Corresponding) |
Parole Chiave: | (+)-usnic acid; MDR-TB; Mycobacterium tuberculosis; Schiff bases; Drug Discovery; |
Settore Scientifico Disciplinare: | Settore CHIM/06 - Chimica Organica Settore CHIM/08 - Chimica Farmaceutica |
Data di pubblicazione: | dic-2018 |
Rivista: | |
Tipologia: | Article (author) |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1002/ardp.201800177 |
Appare nelle tipologie: | 01 - Articolo su periodico |
File in questo prodotto:
File | Descrizione | Tipologia | Licenza | |
---|---|---|---|---|
articolo.pdf | e-pub ahead of print | Publisher's version/PDF | Administrator Richiedi una copia | |
ardp.201800177.pdf | Publisher's version/PDF | Administrator Richiedi una copia |