Synthesis and In Vitro Human Carbonic Anhydrase I and II Inhibition Properties of Some Novel Hydrazone Compounds Containing an Aryl Sulfonate Moiety

Authors : Reşit ÇAKMAK

Pages : 659-669

Doi:10.18185/erzifbed.1132001

View : 18 | Download : 11

Publication Date : 2022-08-31

Article Type : Research Paper

Abstract :The aim of this research was to evaluate the enzyme inhibitory potential of some new hydrazone derivatives bearing an aryl sulfonate moiety against the human carbonic anhydrase isoenzymes I and II (hCA I and II), which were attained from commercial suppliers. In the current study, the structures of targeted molecules (5-8) were characterized by some spectroscopic techniques. The inhibition capacities of the compounds on hCA I and II activities were examined by employing the esterase activity method under in vitro conditions. The IC50 values of the tested molecules were determined in the range of 15.7-135.2 µM against hCA I and in the range of 13.5-76.3 µM against hCA II. Among them, compound 7 exhibited the highest activity against both hCA I and II. The inhibitory activity results of all tested compounds were also compared to the standard drug Acetazolamide (AAZ). It was established that some of the tested molecules showed the inhibitory activities close to AAZ.
Keywords : Aryl sulfonate, hydrazone compound, enzyme inhibitory, human carbonic anhydrase