Benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulfonamides as inhibitors of carbonic anhydrase

Titration Calorimetry Standards and the Precision of Isothermal Titration Calorimetry Data

“…Chemical structures of the ligands numbered 3a-3c have been described previously [27]. Other ligand name abbreviations are: AZM – acetazolamide, MZM – methazolamide, TFMSA – trifluoromethane sulfonamide, CBS – p-carboxy benzene sulfonamide, EZA – ethoxzolamide.…”

Benzenesulfonamides with benzimidazole moieties as inhibitors of carbonic anhydrases I, II, VII, XII and XIII

“…Recently, we have investigated the interaction of several CA isozymes with pyrimidine derivatives such as [(2-pyrimidinylthio)acetyl]benzenesulfonamides 20 , 4-[N-(substituted 4-pyrimidinyl)amino]benzenesulfonamides 21 and thiadiazole derivatives 22 . We have also reported on the synthesis of 2-substituted benzimidazoles N-alkylated with 2-chloro-5-bromoacetylbenzenesulfonamide ( Figure 2, compounds 4(a-j)) and their binding to four CA isozymes, namely CA I, CA II, CA VII and CA XIII 23 .…”

Inhibition and binding studies of carbonic anhydrase isozymes I, II and IX with benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulphonamides

“…The synthesis of benzimidazo[1,2-c] [1,2,3]thiadiazole-7-sulphonamides has been described previously [13]. These compounds are good binders and inhibitors of several CAs.…”

“…Dissociation constants of inhibitors 1a-g binding to hCA I and bovine CA II, purchased from Sigma, determined by ITC are listed in [13]. Table 2.…”

“…In the current study the binding and inhibition of human (h) CA I, hCA II and hCA IX by benzimidazo [1,2-c] [1,2,3]thiadiazole-7-sulphonamides [13] was studied by means of enzyme inhibition. These results were compared to biophysical methods of binding determination, and related to the co-crystal structure of the enzymeinhibitor complex.…”