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

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

doi:10.1002/ardp.201800177

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

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

IRCCS Ospedale San Raffaele

Research output: Contribution to journal › Article › peer-review

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 language	English
Article number	e1800177
Journal	Archiv der Pharmazie
Volume	351
DOIs	https://doi.org/10.1002/ardp.201800177
Publication status	Published - 2018

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title = "Synthesis and antimycobacterial activity of (+)-usnic acid conjugates",

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. {\textcopyright} 2018 Deutsche Pharmazeutische Gesellschaft",

author = "D Cirillo and E Borroni and I Festoso and D Monti and S Romeo and D Mazier and L Verotta",

year = "2018",

doi = "10.1002/ardp.201800177",

language = "English",

volume = "351",

journal = "Archiv der Pharmazie",

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publisher = "Wiley-VCH Verlag",

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T1 - Synthesis and antimycobacterial activity of (+)-usnic acid conjugates

AU - Cirillo, D

AU - Borroni, E

AU - Festoso, I

AU - Monti, D

AU - Romeo, S

AU - Mazier, D

AU - Verotta, L

PY - 2018

Y1 - 2018

N2 - 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

AB - 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

U2 - 10.1002/ardp.201800177

DO - 10.1002/ardp.201800177

M3 - Article

VL - 351

JO - Archiv der Pharmazie

JF - Archiv der Pharmazie

SN - 0365-6233

M1 - e1800177

ER -