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Two novel proton transfer compounds (HAP) + (SAMAL) -and (HBI) + (SAMAL) -.H 2 O were obtained from (E)-4-oxo-4-(4-sulfamoylphenylamino)but-2-enoic acid (HSAMAL) and 2-aminopyridine (AP) or 1H-benzimidazole (BI), respectively. Copper(II) complexes of salts and of HSAMAL have also been prepared. They have been characterized by elemental, spectral, thermal analyses, magnetic measurement and molar conductivity. Human carbonic anhydrase isozymes (hCA I and hCA II) were purified from erythrocytes by using affinity chromatography as 84.40 and 188.71 fold, respectively. The inhibitory effects of synthesized compounds and acetazolamide (AAZ, control compound) on the hydratase and esterase activities of hCA isozymes have been studied as in vitro to find out their antiglaucoma potentials. The inhibition constant (K i ) values of the compounds were in the range of 0.18 ± 0.007 to 10.24 ± 0.014 µmol L -1 for hCA I, and 0.12 ± 0.004 to 130.11 ± 0.021 µmol L -1 for hCA II.

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Novel sulfaguanidines incorporating acridine moiety were synthesized by the reaction of cyclohexane-1,3-dione, sulfaguanidine, and aromatic aldehydes. Synthesis of these compounds was performed in water at room temperature, and their structures were confirmed by using spectral analysis (IR, H-NMR,C-NMR, and HRMS). Human carbonic anhydrase isoenzymes (hCA I and II) were purified from erythrocyte cells with affinity chromatography. hCA I was purified 83.40-fold with a specific activity, 1060.9 EU mg protein, and hCA II was purified 262.32-fold with a specific activity, 3336.8 EU mg protein. The inhibitory effects of newly synthesized sulfaguanidines and acetazolamide, (AAZ) as a control compound, on hydratase and esterase activities of these isoenzymes have been studied in vitro. Synthesized compounds have moderate inhibition potentials on hCA I and hCA II isoenzymes. IC values of compounds for esterase activity are in the range of 118.4 ± 7.0 μM-257.5 ± 5.2 μM for hCA I and 86.7 ± 3.0 μM-249.4 ± 10.2 μM for hCA II, respectively.