Synthesis and antimycobacterial activity of (+)-usnic acid conjugates
Corresponding Author
Daniela Cirillo
Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, Milan, Italy
Correspondence
Dr. Luisella Verotta, Department of Environmental Science and Policy, Università degli Studi di Milano, via C. Golgi 19, 20133 Milano, Italy.
Email: [email protected]
Dr. Daniela Cirillo, Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, via Olgettina 60, 20132 Milano, Italy.
Email: [email protected]
Search for more papers by this authorEmanuele Borroni
Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, Milan, Italy
Search for more papers by this authorIrene Festoso
Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, Milan, Italy
Search for more papers by this authorSergio Romeo
Department of Pharmaceutical Sciences, Università degli Studi di Milano, Milan, Italy
Search for more papers by this authorDominique Mazier
Sorbonne Universités, Centre d'Immunologie et des Maladies Infectieuses, Paris, France
Search for more papers by this authorCorresponding Author
Luisella Verotta
Department of Environmental Science and Policy, Università degli Studi di Milano, Milan, Italy
Consorzio Interuniversitario Nazionale Metodologie e Processi Innovativi di Sintesi, MIlan, Italy
Correspondence
Dr. Luisella Verotta, Department of Environmental Science and Policy, Università degli Studi di Milano, via C. Golgi 19, 20133 Milano, Italy.
Email: [email protected]
Dr. Daniela Cirillo, Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, via Olgettina 60, 20132 Milano, Italy.
Email: [email protected]
Search for more papers by this authorCorresponding Author
Daniela Cirillo
Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, Milan, Italy
Correspondence
Dr. Luisella Verotta, Department of Environmental Science and Policy, Università degli Studi di Milano, via C. Golgi 19, 20133 Milano, Italy.
Email: [email protected]
Dr. Daniela Cirillo, Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, via Olgettina 60, 20132 Milano, Italy.
Email: [email protected]
Search for more papers by this authorEmanuele Borroni
Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, Milan, Italy
Search for more papers by this authorIrene Festoso
Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, Milan, Italy
Search for more papers by this authorSergio Romeo
Department of Pharmaceutical Sciences, Università degli Studi di Milano, Milan, Italy
Search for more papers by this authorDominique Mazier
Sorbonne Universités, Centre d'Immunologie et des Maladies Infectieuses, Paris, France
Search for more papers by this authorCorresponding Author
Luisella Verotta
Department of Environmental Science and Policy, Università degli Studi di Milano, Milan, Italy
Consorzio Interuniversitario Nazionale Metodologie e Processi Innovativi di Sintesi, MIlan, Italy
Correspondence
Dr. Luisella Verotta, Department of Environmental Science and Policy, Università degli Studi di Milano, via C. Golgi 19, 20133 Milano, Italy.
Email: [email protected]
Dr. Daniela Cirillo, Division of Infectious Diseases, Immunology and Transplantation, Emerging Bacterial Pathogens Unit, San Raffaele Scientific Institute, via Olgettina 60, 20132 Milano, Italy.
Email: [email protected]
Search for more papers by this authorAbstract
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.
CONFLICT OF INTEREST
The authors declare no conflict of interest.
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