Synthesis of novel benzenesulfamide derivatives with inhibitory activity against human cytosolic carbonic anhydrase I and II and Vibrio cholerae α- and β-class enzymes |
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| Authors: | Silvia Bua Emanuela Berrino Sonia Del Prete Vallabhaneni S Murthy Vijayaparthasarathi Vijayakumar Yasinalli Tamboli |
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| Institution: | 1. NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Sesto Fiorentino (Florence), Italy;2. School of Advanced Sciences, Center for Organic and Medicinal Chemistry, VIT University, Vellore, India |
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| Abstract: | The synthesis of a new series of sulfamides incorporating ortho-, meta, and para-benzenesulfamide moieties is reported, which were investigated for the inhibition of two human (h) isoforms of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), hCA I and II, and two Vibrio cholerae enzymes, belonging to the α- and β-CA classes (VchCAα, VchCAβ). The compounds were prepared by using the “tail approach”, aiming to overcome the scarcity of selective inhibition profiles associated to CA inhibitors belonging to the zinc binders. The built structure–activity relationship showed that the incorporation of benzhydryl piperazine tails on a phenyl sulfamide scaffold determines rather good efficacies against hCA I and VchCAα, with several compounds showing KIs?
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| Keywords: | Carbonic anhydrase inhibitors (CAIs) sulfamides structure–activity relationship (SAR) Vibrio cholerae |
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