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, Ufuk; Yıldırım, Alper; Taslimi, Parham; Çelik, Seda Tuncel; Gülçin, İlhami; Supuran, Claudiu T; Çelik, Murat. - 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.
2018
32
0
0
Goal 3: Good health and well-being
Atmaca, Ufuk; Yıldırım, Alper; Taslimi, Parham; Çelik, Seda Tuncel; Gülçin, İlhami; Supuran, Claudiu T; Çelik, Murat...espandi
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1308165
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