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Appraisal of anti-protozoan activity of nitroaromatic benzenesulfonamides inhibiting carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani.
Nocentini, Alessio; Osman, Sameh M; Almeida, Igor A; Cardoso, Veronica; Alasmary, Fatmah Ali S; AlOthman, Zeid; Vermelho, Alane B; Gratteri, Paola; Supuran, Claudiu T.
Afiliación
  • Nocentini A; a Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences , University of Florence , Sesto Fiorentino , Italy.
  • Osman SM; b Department of Chemistry, College of Science , King Saud University , Riyadh , Saudi Arabia.
  • Almeida IA; c Department of Natural Products and Food, School of Pharmacy , Federal University of Rio de Janeiro , Rio de Janeiro , Brazil.
  • Cardoso V; d BIOINOVAR - Biotechnology Laboratories: Biocatalysis, Bioproducts and Bioenergy, Institute of Microbiology Paulo de Góes , Federal University of Rio de Janeiro , Rio de Janeiro , Brazil.
  • Alasmary FAS; b Department of Chemistry, College of Science , King Saud University , Riyadh , Saudi Arabia.
  • AlOthman Z; b Department of Chemistry, College of Science , King Saud University , Riyadh , Saudi Arabia.
  • Vermelho AB; d BIOINOVAR - Biotechnology Laboratories: Biocatalysis, Bioproducts and Bioenergy, Institute of Microbiology Paulo de Góes , Federal University of Rio de Janeiro , Rio de Janeiro , Brazil.
  • Gratteri P; a Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences , University of Florence , Sesto Fiorentino , Italy.
  • Supuran CT; a Department of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences , University of Florence , Sesto Fiorentino , Italy.
J Enzyme Inhib Med Chem ; 34(1): 1164-1171, 2019 Dec.
Article en En | MEDLINE | ID: mdl-31219348
Chagas disease and leishmaniasis are neglected tropical disorders caused by the protozoans Trypanosoma cruzi and Leishmania spp. Carbonic anhydrases (CAs, EC 4.2.1.1) from these protozoans (α-TcCA and ß-LdcCA) have been validated as promising targets for chemotherapic interventions. Many anti-protozoan agents, such as nitroimidazoles, nifurtimox, and benznidazole possess a nitro aromatic group in their structure which is crucial for their activity. As a continuation of our previous work on N-nitrosulfonamides as anti-protozoan agents, we investigated benzenesulfonamides bearing a nitro aromatic moiety against TcCA and LdcCA, observing selective inhibitions over human off-target CAs. Selected derivatives were assessed in vitro in different developmental stages of T. cruzi and Leishmania spp. A lack of significant growth inhibition has been found, which has been connected to the low permeability of this class of derivatives through cell membranes. Further strategies necessarily need to be designed for targeting Chagas disease and leishmaniasis with nitro-containing CA inhibitors.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Trypanosoma cruzi / Leishmania donovani / Inhibidores de Anhidrasa Carbónica / Anhidrasas Carbónicas / Antiprotozoarios Límite: Humans Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Trypanosoma cruzi / Leishmania donovani / Inhibidores de Anhidrasa Carbónica / Anhidrasas Carbónicas / Antiprotozoarios Límite: Humans Idioma: En Revista: J Enzyme Inhib Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Reino Unido