A new class of quinazoline-sulfonamides acting as efficient inhibitors against the α-carbonic anhydrase from Trypanosoma cruzi

Ahmed M. AlafeefyDepartment of Pharmaceutical Chemistry, College of Pharmacy, Salman bin Abdulaziz University, Al-Kharj, Saudi Arabia, Correspondence[email protected]

Mariangela CerusoPolo Scientifico, Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Sesto Fiorentino, Florence, Italy, Correspondence[email protected]

Nabila A. Al-JaberChemistry Department, College of Science, King Saud University, Riyadh, Saudi Arabia,

Seppo ParkkilaSchool of Medicine and Fimlab Ltd, University of Tampere, Tampere, Finland,

Alane Beatriz VermelhoLaboratório Proteases de Microrganismos, Instituto de Microbiologia Paulo de Góes, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil, and

Claudiu T. SupuranPolo Scientifico, Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Sesto Fiorentino, Florence, Italy, ;Neurofarba Department, Section of Pharmaceutical and Nutriceutical Sciences, Università degli Studi di Firenze, Florence, Italy

Figures & data

Scheme 1. Synthesis of the 2,3,5,6 and/or 8-substituted-4-oxoquinazoline derivatives 8a–h and their bioisosters 4-thioxoquinazoline derivatives 9a–e.

Table 1. Inhibition data of quinazoline-sulfonamides 8a–h, 9a–e and acetazolamide AAZ (as standard inhibitor) against human (h) isoforms hCA I, II (cytosolic) and the protozoan enzyme TcCA by a stopped-flow CO₂ hydrase assay (13). The selectivity ratios are also reported.

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A new class of quinazoline-sulfonamides acting as efficient inhibitors against the α-carbonic anhydrase from Trypanosoma cruzi

Table 1. Inhibition data of quinazoline-sulfonamides 8a–h, 9a–e and acetazolamide AAZ (as standard inhibitor) against human (h) isoforms hCA I, II (cytosolic) and the protozoan enzyme TcCA by a stopped-flow CO₂ hydrase assay (13). The selectivity ratios are also reported.

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A new class of quinazoline-sulfonamides acting as efficient inhibitors against the α-carbonic anhydrase from Trypanosoma cruzi

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Table 1. Inhibition data of quinazoline-sulfonamides 8a–h, 9a–e and acetazolamide AAZ (as standard inhibitor) against human (h) isoforms hCA I, II (cytosolic) and the protozoan enzyme TcCA by a stopped-flow CO2 hydrase assay (13). The selectivity ratios are also reported.

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Table 1. Inhibition data of quinazoline-sulfonamides 8a–h, 9a–e and acetazolamide AAZ (as standard inhibitor) against human (h) isoforms hCA I, II (cytosolic) and the protozoan enzyme TcCA by a stopped-flow CO₂ hydrase assay (13). The selectivity ratios are also reported.