Investigation of the inhibitory effeckts of sulfaguanidine moiety including dioxoacridine derivatives on human carbonic anhydrase isoenzymes

Carbonic anhydrases (E.C. 4.2.1.1.) are family of zinc metalloenzymes that catalyze the reversible hydration of carbon dioxide in a two-stop reaction to yield bicarbonate and proton. The isoenzymes of human eye are CA-I, CAII and CA-IV. Carbonic anhydrase inhibitors, which reduce aqueous production with a corresponding decrease in intraocular pressure (IOP), have been used as ocular hypotensive agents for the treatment of glaucoma. In this study, new carbonic anhydrase inhibitors's effects on carbonic anhydrase enzyme as candidates for treatment of glaucoma were investigated. First, carbonic anhydrase enzymes from human erythrocyte were purifed using affinity gel and all of the investigations were carried out with these enzymes. Later, inhibition effects of these new compounds (1, 2, 3, 4, 5 ) on human carbonic anhydrase enzymes (HCA I and HCA II) were investigated in vitro. In the studies, it was taken advantage of esterase activites for determining of carbonic anhydrase activitates. It was observed that compounds (1, 2, 3, 4, 5) showed inhibition effect on HCA esterase activity. Drawing % activity-[I] graphs for compounds showing inhibition effects. Key Words: Glaucoma, Carbonic Anhydrase, Sulfaguanidine and Dioxoacridine