Article ID Journal Published Year Pages File Type
1369540 Bioorganic & Medicinal Chemistry Letters 2016 5 Pages PDF
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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Physical Sciences and Engineering Chemistry Organic Chemistry
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