In this study, we aimed to determine the inhibition effects of novel synthesized sulfamates (2a-g), sulfonamides (3b-f). carbonyl sulfonamides (3h and i). and carbonyl sulfamates (4h and 4i), which were tested against two human cytosolic carbonic anhydrase I and II isozymes (hCA I and II) and acetylcholinesterase (AChE) enzyme. For inhibition properties of allylic sulfamates, the half maximal inhibitory concentration (IC50) and inhibition constant (K-i) were calculated for each novel compounds. The allylic sulfamates showed that K-i values are in the range of 187.33-510.31 pM for hCA I. 104.22 -290.09 pM against hCA II, and 12.73-103.63 pM against AChE. The results demonstrated that all newly synthesized compounds had shown effective inhibition against hCA I and II isoenzymes and AChE enzyme.
Intermolecular amination of allylic and benzylic alcohols leads to effective inhibitions of acetylcholinesterase enzyme and carbonic anhydrase I and II isoenzymes / Atmaca, U., Yıldırım, A., Taslimi, P., Çelik, S.T., Gülçin, İ., Supuran, C.T., Çelik, M.. - In: JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY. - ISSN 1095-6670. - ELETTRONICO. - 32:(2018), pp. 0-0. [10.1002/jbt.22173]
Intermolecular amination of allylic and benzylic alcohols leads to effective inhibitions of acetylcholinesterase enzyme and carbonic anhydrase I and II isoenzymes
Supuran, Claudiu T;
2018
Abstract
In this study, we aimed to determine the inhibition effects of novel synthesized sulfamates (2a-g), sulfonamides (3b-f). carbonyl sulfonamides (3h and i). and carbonyl sulfamates (4h and 4i), which were tested against two human cytosolic carbonic anhydrase I and II isozymes (hCA I and II) and acetylcholinesterase (AChE) enzyme. For inhibition properties of allylic sulfamates, the half maximal inhibitory concentration (IC50) and inhibition constant (K-i) were calculated for each novel compounds. The allylic sulfamates showed that K-i values are in the range of 187.33-510.31 pM for hCA I. 104.22 -290.09 pM against hCA II, and 12.73-103.63 pM against AChE. The results demonstrated that all newly synthesized compounds had shown effective inhibition against hCA I and II isoenzymes and AChE enzyme.
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