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Evaluation of acetylcholinesterase and carbonic anhydrase inhibition profiles of 1,2,3,4,6‐pentasubstituted‐4‐hydroxy‐cyclohexanes
Authors:Umit M Kocyigit  Parham Taslimi  Hayreddin Gezegen  ?lhami Gulçin  Mustafa Ceylan
Institution:1. Vocational School of Health Services, Cumhuriyet University, Sivas, Turkey;2. Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, Turkey;3. Department of Nutrition and Dietetics, Faculty of Health Sciences, Cumhuriyet University, Sivas, Turkey;4. Department of Chemistry, Faculty of Arts and Sciences, Gaziosmanpasa University, Tokat, Turkey
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.
Keywords:acetylcholinesterase  carbonic anhydrase  domino reactions  enzyme inhibition pentasubstituted cyclohexanol
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