info:eu-repo/semantics/article
Anti-tubercular and antioxidant activities of C-glycosyl carbonic anhydrase inhibitors: towards the development of novel chemotherapeutic agents against Mycobacterium tuberculosis
Fecha
2016-05Registro en:
Zaro, Maria Jose; Bortolotti, Ana; Riafrecha, Leonardo Ezequiel; Concellón, Analía; Morbidoni, Héctor Ricardo; et al.; Anti-tubercular and antioxidant activities of C-glycosyl carbonic anhydrase inhibitors: towards the development of novel chemotherapeutic agents against Mycobacterium tuberculosis; Taylor & Francis Ltd; Journal of Enzyme Inhibition and Medicinal Chemistry; 31; 5-2016; 1726-1730
1475-6366
CONICET Digital
CONICET
Autor
Zaro, Maria Jose
Bortolotti, Ana
Riafrecha, Leonardo Ezequiel
Concellón, Analía
Morbidoni, Héctor Ricardo
Colinas, Pedro Alfonso
Resumen
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.