Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369540 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
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 KI’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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Related Topics
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Authors
Raed Yaseen, Deniz Ekinci, Murat Senturk, Alhamzah Dh. Hameed, Syed Ovais, Pooja Rathore, Mohammed Samim, Kalim Javed, Claudiu T. Supuran,