Anti-tubercular and antioxidant activities of C-glycosyl carbonic anhydrase inhibitors: towards the development of novel chemotherapeutic agents against Mycobacterium tuberculosis |
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| Authors: | María J Zaro Ana Bortolotti Leonardo E Riafrecha Analía Concellón |
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| Institution: | 1. CIDCA (Centro de Investigación y Desarrollo en Criotecnología de Alimentos, CCT La Plata-CONICET, UNLP), La Plata, Argentina,;2. Laboratorio de Microbiologia Molecular, Cátedra de Microbiología, Virología y Parasitología;3. Facultad de Ciencias Médicas, Universidad Nacional de Rosario, Rosario, Argentina, and;4. LADECOR CONICET, Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, La Plata, Argentina |
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| Abstract: | During the treatment of tuberculosis infection, oxidative stress due to anti-tubercular drugs may result in tissue inflammation. It was suggested that treatment with antioxidant drugs could be beneficial as an adjunct to anti-tuberculosis drug therapy. Recently our group has shown that several C-glycosides are inhibitors of Mycobacterium tuberculosis β-carbonic anhydrases (CAs, EC 4.2.1.1). In an effort to develop novel chemotherapeutic agents against tuberculosis, the anti-tubercular and antioxidant activities of a series of C-glycosides containing the phenol or the methoxyaryl moiety were studied. Many compounds showed inhibition of growth of M. tuberculosis H37Rv strain and good antioxidant ability. A glycomimetic incorporating the 3-hydroxyphenyl moiety showed the best activity profile and therefore this functionality represents lead for the development of novel anti-tubercular agents with dual mechanisms of action. |
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| Keywords: | Dual mechanism glycomimetic tuberculosis |
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