2. Academic Validation
  3. New Dihydrothiazole Benzensulfonamides: Looking for Selectivity toward Carbonic Anhydrase Isoforms I, II, IX, and XII

New Dihydrothiazole Benzensulfonamides: Looking for Selectivity toward Carbonic Anhydrase Isoforms I, II, IX, and XII

  • ACS Med Chem Lett. 2020 Feb 13;11(5):852-856. doi: 10.1021/acsmedchemlett.9b00644.
Rita Meleddu 1,  Simona Distinto 1,  Filippo Cottiglia 1,  Rossella Angius 2,  Pierluigi Caboni 1,  Andrea Angeli 3,  Claudia Melis 1,  Serenella Deplano 1,  Stefano Alcaro 4,  Francesco Ortuso 4,  Claudiu T Supuran 3,  Elias Maccioni 1
Affiliations

Affiliations

  • 1 Department of Life and Environmental Sciences, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.
  • 2 Laboratorio NMR e Tecnologie Bioanalitiche, Sardegna Ricerche, 09010 Pula, CA, Italy.
  • 3 Dipartimento NEUROFARBA, Sezione di Scienze Farmaceutiche, Università degli Studi di Firenze, Sesto Fiorentino, 50139 Florence, Italy.
  • 4 Dipartimento di Scienze della Salute, Università Magna Graecia di Catanzaro, Campus "S. Venuta", Viale Europa, 88100 Catanzaro, Italy.
PMID: 32435395 DOI: 10.1021/acsmedchemlett.9b00644
Abstract

In the present study we investigated the structure-activity relationships of a new series of 4-[(3-ethyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides (EMAC10101a-m). All synthesized compounds, with the exception of compound EMAC10101k, preferentially inhibit off-target hCA II isoform. Within the series, compound EMAC10101d, bearing a 2,4-dichorophenyl substituent in position 4 of the dihydrothiazole ring, was the most potent and selective toward hCA II with an inhibitory activity in the low nanomolar range.

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