Appraisal of anti-protozoan activity of nitroaromatic benzenesulfonamides inhibiting carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani

Alessio NocentiniDepartment of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Sesto Fiorentino, Italy; View further author information

Sameh M. OsmanDepartment of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia; View further author information

Igor A. RodriguesDepartment of Natural Products and Food, School of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil; View further author information

Veronica S. CardosoBIOINOVAR – Biotechnology Laboratories: Biocatalysis, Bioproducts and Bioenergy, Institute of Microbiology Paulo de Góes, Federal University of Rio de Janeiro, Rio de Janeiro, BrazilView further author information

Fatmah Ali S. AlasmaryDepartment of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia; View further author information

Zeid AlOthmanDepartment of Chemistry, College of Science, King Saud University, Riyadh, Saudi Arabia; View further author information

Alane B. VermelhoBIOINOVAR – Biotechnology Laboratories: Biocatalysis, Bioproducts and Bioenergy, Institute of Microbiology Paulo de Góes, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil

http://orcid.org/0000-0001-5926-4172 View further author information

Paola GratteriDepartment of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Sesto Fiorentino, Italy; Correspondence[email protected]
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Claudiu T. SupuranDepartment of Neuroscience, Psychology, Drug Research and Child's Health, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Sesto Fiorentino, Italy; Correspondence[email protected]

http://orcid.org/0000-0003-4262-0323 View further author information

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Appraisal of anti-protozoan activity of nitroaromatic benzenesulfonamides inhibiting carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani

Table 1. Inhibition data of TcCA, LdCA and human CA I and II with sulfonamides reported here and the standard inhibitor acetazolamide (AAZ) by a stopped flow CO₂ hydrase assay.

Table 2. Selectivity index (SI) for target protozoan CAs over hCA I and II.

Table 3. Minimum inhibitory concentration (MIC), IC₅₀ values derived from growth inhibition assays of T. cruzi Dm 28c and Y, determination of cytotoxicity (CC₅₀), selectivity index (SI₅₀) of compounds 4, 6, 8, 10, 11, 17, 18, 19, 21, and 24.

Table 4. Minimum inhibitory concentration (MIC), IC₅₀ values derived from growth inhibition assays of L. amazonensis and L. infantum, determination of cytotoxicity (CC₅₀) and selectivity index (SI₅₀) of compounds 4, 6, 8, 10, 11, 17, 18, 19, 21, and 24.

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Appraisal of anti-protozoan activity of nitroaromatic benzenesulfonamides inhibiting carbonic anhydrases from Trypanosoma cruzi and Leishmania donovani

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Table 1. Inhibition data of TcCA, LdCA and human CA I and II with sulfonamides reported here and the standard inhibitor acetazolamide (AAZ) by a stopped flow CO2 hydrase assay.

Table 2. Selectivity index (SI) for target protozoan CAs over hCA I and II.

Table 3. Minimum inhibitory concentration (MIC), IC50 values derived from growth inhibition assays of T. cruzi Dm 28c and Y, determination of cytotoxicity (CC50), selectivity index (SI50) of compounds 4, 6, 8, 10, 11, 17, 18, 19, 21, and 24.

Table 4. Minimum inhibitory concentration (MIC), IC50 values derived from growth inhibition assays of L. amazonensis and L. infantum, determination of cytotoxicity (CC50) and selectivity index (SI50) of compounds 4, 6, 8, 10, 11, 17, 18, 19, 21, and 24.

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Table 1. Inhibition data of TcCA, LdCA and human CA I and II with sulfonamides reported here and the standard inhibitor acetazolamide (AAZ) by a stopped flow CO₂ hydrase assay.

Table 3. Minimum inhibitory concentration (MIC), IC₅₀ values derived from growth inhibition assays of T. cruzi Dm 28c and Y, determination of cytotoxicity (CC₅₀), selectivity index (SI₅₀) of compounds 4, 6, 8, 10, 11, 17, 18, 19, 21, and 24.

Table 4. Minimum inhibitory concentration (MIC), IC₅₀ values derived from growth inhibition assays of L. amazonensis and L. infantum, determination of cytotoxicity (CC₅₀) and selectivity index (SI₅₀) of compounds 4, 6, 8, 10, 11, 17, 18, 19, 21, and 24.