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  • Title: Pyridazinone substituted benzenesulfonamides as potent carbonic anhydrase inhibitors.
    Author: Yaseen R, Ekinci D, Senturk M, Hameed AD, Ovais S, Rathore P, Samim M, Javed K, Supuran CT.
    Journal: Bioorg Med Chem Lett; 2016 Feb 15; 26(4):1337-41. PubMed ID: 26804228.
    Abstract:
    A series of sulfonamide derivatives (2a-l) incorporating substituted pyridazinone moieties were investigated for the inhibition of two human cytosolic carbonic anhydrase isoforms, hCA I and hCA II. All these compounds, together with the clinically used sulfonamide acetazolamide were investigated as inhibitors of the physiologically relevant isozymes I and II. These sulfonamides showed very strong inhibition against all these isoforms with K(I)'s in the range of 0.98-8.5 nM which makes such molecules possible to be used as leads for discovery of novel effective CA inhibitors targeting other isoforms with medicinal chemistry applications.
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