Anti-tubercular and antioxidant activities of C-glycosyl carbonic anhydrase inhibitors: Towards the development of novel chemotherapeutic agents against Mycobacterium tuberculosis

ZARO, MJ; BORTOLLOTI, A; RIAFRECHA, LE; CONCELLON, ANALIA; MORBIDONI, HR; COLINAS, P

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

TAYLOR & FRANCIS LTD

Lugar: Londres; Año: 2016 vol. 31 p. 1726 - 1730

1475-6366

During the treatment of tuberculosis infection, oxidative stress may result in tissue inflammation due to anti-tubercular drugs. 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 -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.