Volume 31, Issue 9 e21938
RESEARCH ARTICLE

Evaluation of acetylcholinesterase and carbonic anhydrase inhibition profiles of 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes

Umit M. Kocyigit

Corresponding Author

Umit M. Kocyigit

Vocational School of Health Services, Cumhuriyet University, Sivas, Turkey

Correspondence

Umit M. Kocyigit, Vocational School of Health Services, Cumhuriyet University, 58140 Sivas, Turkey.

E-mail: [email protected]

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Parham Taslimi

Parham Taslimi

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

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Hayreddin Gezegen

Hayreddin Gezegen

Department of Nutrition and Dietetics, Faculty of Health Sciences, Cumhuriyet University, Sivas, Turkey

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İlhami Gulçin

İlhami Gulçin

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

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Mustafa Ceylan

Mustafa Ceylan

Department of Chemistry, Faculty of Arts and Sciences, Gaziosmanpasa University, Tokat, Turkey

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First published: 14 June 2017
Citations: 42

Abstract

Carbonic anhydrase (CA; EC 4.2.1.1) is used for remedial purposes for several years, as there is significant focus on expanding more new activators (CAAs) and high affinity inhibitors. Alzheimer′s disease and other similar ailments such as dementia and vascular dementia with Lewy bodies reduce cholinergic activity in the important areas involved in cognition and memory. Prevalent drugs for the symptomatic therapy of dementia are significant in increasing the associated cholinergic deficiency by inhibiting acetylcholinesterase (AChE). These six-membered carbocycles showed nice inhibitory action against AChE and human carbonic anhydrase (hCA) II and I isoforms. The hCA I, II, and AChE were efficiently inhibited by these molecules, with Ki values in the range of 6.70–35.85 nM for hCA I, 18.77–60.84 nM for hCA II, and 0.74–4.60 for AChE, respectively.

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