Volume 31, Issue 9 e21931
RESEARCH ARTICLE

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

Parham Taslimi

Parham Taslimi

Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, 25240 Turkey

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Sabiya Osmanova

Sabiya Osmanova

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, 1029 Azerbaijan

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İlhami Gulçin

Corresponding Author

İlhami Gulçin

Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, 25240 Turkey

Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia

Correspondence

Ilhami Gulcin

E-mails: [email protected], [email protected]

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Sabira Sardarova

Sabira Sardarova

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, 1029 Azerbaijan

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Vagif Farzaliyev

Vagif Farzaliyev

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, 1029 Azerbaijan

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Afsun Sujayev

Afsun Sujayev

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, 1029 Azerbaijan

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Ruya Kaya

Ruya Kaya

Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, 25240 Turkey

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Fatma Koc

Fatma Koc

Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, 25240 Turkey

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Sukru Beydemir

Sukru Beydemir

Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, 26470 Turkey

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Saleh H. Alwasel

Saleh H. Alwasel

Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia

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Omer Irfan Kufrevioglu

Omer Irfan Kufrevioglu

Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, 25240 Turkey

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First published: 22 May 2017
Citations: 50

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 Ki 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 Ki 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 Ki values of 397.03 ± 31.66 and 210.21 ± 15.98 nM, respectively.

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