Investigation of novel dioxoacridine nitrogenous derivates as new carbonic anhydrase inhibitors

In this study, the inhibitory effect of new synthesized acridine sulphoguanidine derivate compounds on carbonic anhydrase is isoenzymes that is hCA I and hCA II were investigated. In this direction, at first hCA I and hCA II isoenzymes were purified from human erythrocytes with affinity chromatography and purity of the enzymes was checked with SDS-PAGE electrophoresis. Later, the inhibitory effects of the compounds 1-5 on hCA I and hCA II isoenzymes were determined. To determine inhibitory effect of this compounds the hydratase and esterase activities of carbonic anhydrase enzyme were measured. According to the results, %Activity-[I] graphics were drawn and the IC50 values were calculated. Lastly, No inhibitory effects of the 1-5 compounds weren?t observed on hydratase activities of hCA I and hCA II isoenzymes. But these compounds were observed inhibitory effects on the esterase activities of hCA I and hCA II isoenzymes. The IC50 values of compounds for esterase activity varied between 118,4-257,5 ?M for hCA I and 86,7-177,2 ?M for hCA II, respectively. Key Words: Acridine Compounds, Carbonic Anhydrase, Glaucoma, IC50 Values, Sulfonamides.