title: Anti-tubercular and antioxidant activities of C-glycosyl carbonic anhydrase inhibitors: towards the development of novel chemotherapeutic agents against Mycobacterium tuberculosis.
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.
authors.affiliation: a CIDCA (Centro de Investigación y Desarrollo en Criotecnología de Alimentos, CCT La Plata-CONICET, UNLP) , La Plata , Argentina .
authors.forename: María J
authors.initials: MJ
authors.lastname: Zaro
authors.affiliation: b Laboratorio de Microbiologia Molecular , Cátedra de Microbiología, Virología y Parasitología; Facultad de Ciencias Médicas, Universidad Nacional de Rosario , Rosario , Argentina , and.
authors.forename: Ana
authors.initials: A
authors.lastname: Bortolotti
authors.affiliation: c LADECOR CONICET, Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata , La Plata , Argentina.
authors.forename: Leonardo E
authors.initials: LE
authors.lastname: Riafrecha
authors.affiliation: a CIDCA (Centro de Investigación y Desarrollo en Criotecnología de Alimentos, CCT La Plata-CONICET, UNLP) , La Plata , Argentina .
authors.forename: Analía
authors.initials: A
authors.lastname: Concellón
authors.affiliation: b Laboratorio de Microbiologia Molecular , Cátedra de Microbiología, Virología y Parasitología; Facultad de Ciencias Médicas, Universidad Nacional de Rosario , Rosario , Argentina , and.
authors.forename: Héctor R
authors.initials: HR
authors.lastname: Morbidoni
authors.affiliation: c LADECOR CONICET, Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata , La Plata , Argentina.
authors.forename: Pedro A
authors.initials: PA
authors.lastname: Colinas
mesh_terms: D000975:Antioxidants / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000494:pharmacology*; D002257:Carbonic Anhydrase Inhibitors / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*
chemical_list: D000975:Antioxidants; D000995:Antitubercular Agents; D002257:Carbonic Anhydrase Inhibitors
keywords: Dual mechanism; glycomimetic; tuberculosis