Evaluation of acetylcholinesterase and carbonic anhydrase inhibition profiles of 1,2,3,4,6-pentasubstituted-4-hydroxy-cyclohexanes
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]
Search for more papers by this authorParham Taslimi
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey
Search for more papers by this authorHayreddin Gezegen
Department of Nutrition and Dietetics, Faculty of Health Sciences, Cumhuriyet University, Sivas, Turkey
Search for more papers by this authorİlhami Gulçin
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey
Search for more papers by this authorMustafa Ceylan
Department of Chemistry, Faculty of Arts and Sciences, Gaziosmanpasa University, Tokat, Turkey
Search for more papers by this authorCorresponding 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]
Search for more papers by this authorParham Taslimi
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey
Search for more papers by this authorHayreddin Gezegen
Department of Nutrition and Dietetics, Faculty of Health Sciences, Cumhuriyet University, Sivas, Turkey
Search for more papers by this authorİlhami Gulçin
Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey
Search for more papers by this authorMustafa Ceylan
Department of Chemistry, Faculty of Arts and Sciences, Gaziosmanpasa University, Tokat, Turkey
Search for more papers by this authorAbstract
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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