Intermolecular amination of allylic and benzylic alcohols leads to effective inhibitions of acetylcholinesterase enzyme and carbonic anhydrase I and II isoenzymes.

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 (Ki ) were calculated for each novel compounds. The allylic sulfamates showed that Ki 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.

journal_name

J Biochem Mol Toxicol

authors

Atmaca U,Yıldırım A,Taslimi P,Çelik ST,Gülçin İ,Supuran CT,Çelik M

doi

10.1002/jbt.22173

subject

Has Abstract

pub_date

2018-08-01 00:00:00

pages

e22173

issue

8

eissn

1095-6670

issn

1099-0461

journal_volume

32

pub_type

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