Carbonic anhydrase IX (CA IX) is a target for hypoxic cancer therapies, and the discovery of CA IX selective ligands is imperative for the development of these agents. Primary sulfonamides are broad specificity inhibitors of CA enzymes, while secondary sulfonamides are generally poor CA inhibitors. However, saccharin, a cyclic secondary sulfonamide, has unusually good inhibition of CA IX (Ki = ...

The mechanism of sulfonamide cleavage of PNU-109112, a potent HIV-1 protease inhibitor, by glutathione-S-transferase (GST) was investigated in the presence of reduced GSH. GST-catalyzed sulfonamide cleavage takes place via the nucleophilic attack of GSH on the pyridine moiety of the substrate with formation of the GS-para-CN-pyridinyl conjugate, the corresponding amine, and sulfur dioxide. Stru...

Studies previously reported on the mode of action of sulfonamides on bacteria showed that the inhibition of respiratory enzymes of the bacteria caused a proportional inhibition of the growth of Streptococcus pyogenes and pneumococcus, type I. This conclusion was based on simultaneous measurements, at various time intervals, of the increase in the number of bacteria (and the mg of bacterial nitr...

The bacteriostatic action of 2-chloro-4-aminobenzoic acid (2-Cl-PAB) was found by Wyss, Rubin, and Strandskov (1943) to be completely reversed by p-aminobenzoic acid. This, according to the theory of Woods (1940) that p-aminobenzoic acid is a specific antagonist for sulfanilamide, classified the bacteriostatic action of 2-Cl-PAB as sulfonamide activity. The bacteriostatic action of this compoun...

new sulfonamide and amide derivatives containing coumarin moieties; oxo-2h-chromen-sulfamoylphenylacetamides and oxo-2h-chromen-arylacetamides were synthesized starting from diverse 2-chloroacetamide derivatives and a wide range of coumarins. the structures of the obtained compounds were elucidated by ir and nmr spectra and also analytical elemental analysis. in the next step, the above mention...