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Discovery of potent carbonic anhydrase, acetylcholinesterase, and butyrylcholinesterase enzymes inhibitors: The new amides and thiazolidine-4-ones synthesized on an acetophenone base.

Authors :
Taslimi, Parham
Osmanova, Sabiya
Gulçin, İlhami
Sardarova, Sabira
Farzaliyev, Vagif
Sujayev, Afsun
Kaya, Ruya
Koc, Fatma
Beydemir, Sukru
Alwasel, Saleh H.
Kufrevioglu, Omer Irfan
Source :
Journal of Biochemical & Molecular Toxicology; Sep2017, Vol. 31 Issue 9, pn/a-N.PAG, 7p
Publication Year :
2017

Abstract

Compounds containing nitrogen and sulfur atoms can be widely used in various fields, including industry, medicine, biotechnology, and chemical technology. Among them, amides of acids and heterocyclic compounds have an important place. These amides and thiazolidine-4-ones showed good inhibitory action against butyrylcholinesterase (BChE), acetylcholinesterase (AChE), and human carbonic anhydrase isoforms. AChE exists at high concentrations in the brain and red blood cells. BChE is an important enzyme that is plentiful in the liver, and it is released into the blood in a soluble form. They were demonstrated to have effective inhibition profiles with K<subscript>i</subscript> values of 23.76-102.75 nM against hCA I, 58.92-136.64 nM against hCA II, 1.40-12.86 nM against AChE, and 9.82-52.77 nM against BChE. On the other hand, acetazolamide showed K<subscript>i</subscript> value of 482.63 ± 56.20 nM against hCA I, and 1019.60 ± 163.70 nM against hCA II. Additionally, Tacrine inhibited AChE and BChE, showing K<subscript>i</subscript> values of 397.03 ± 31.66 and 210.21 ± 15.98 nM, respectively. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
10956670
Volume :
31
Issue :
9
Database :
Complementary Index
Journal :
Journal of Biochemical & Molecular Toxicology
Publication Type :
Academic Journal
Accession number :
124972283
Full Text :
https://doi.org/10.1002/jbt.21931