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

Avermectins are used worldwide as antiparasitic drugs in the field of veterinary medicine and as agricultural pesticides and insecticides. Carbonic anhydrase (CA, E.C. 4.2.1.1) is a zinccontaining metalloenzyme that catalyzes the reversible hydration of carbon dioxide (CO 2 ) to yield protons (H + ) and bicarbonate (HCO 3 − ). In this study, some avermectins, including abamectin, doramectin, eprinomectin, and moxidectin, were investigated for in vitro inhibitory effects on the CA enzyme purified from goat liver, which was purified (125.00-fold) using sepharose 4B-

Section: Resultsmentioning

confidence: 99%

The toxicological effects of some avermectins on goat liver carbonic anhydrase enzyme

Çağlayan

Gülçın

2017

“…The extension of AChE inhibitors, with anticipation of fewer side effects, can be a more rational therapeutic strategy for AD . AChE is a key enzyme splitting the neurotransmitter ACh in cholinergic synapsis into acetic acid and choline .…”

Section: Discussionmentioning

confidence: 99%

Novel N‐propylphthalimide‐ and 4‐vinylbenzyl‐substituted benzimidazole salts: Synthesis, characterization, and determination of their metal chelating effects and inhibition profiles against acetylcholinesterase and carbonic anhydrase enzymes

Sarı

Aktaş

Taslimi

et al. 2017

Self Cite

“…[25][26][27][28][29] In this study, we have performed the synthesis of well-defined novel amide of 1,1-bis-(carboxymethylthio)-1-arylethanes derivatives (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11). [25][26][27][28][29] In this study, we have performed the synthesis of well-defined novel amide of 1,1-bis-(carboxymethylthio)-1-arylethanes derivatives (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11).…”

Section: Introductionmentioning

confidence: 99%

Novel amides of 1,1‐bis‐(carboxymethylthio)‐1‐arylethanes: Synthesis, characterization, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase inhibitory properties

Taslimi

Osmanova

Çağlayan

et al. 2018

Self Cite

The thiolation reaction was carried out in a benzene solution at 80°C and p-substituted ketones and mercaptoacetic acid in a molar ratio (1:4) of in the presence of a catalytic amount of toluene sulfonic acids. The enzyme inhibition activities of the novel amides of 1,1-bis-(carboxymethylthio)-1-arylethanes derivatives were investigated. These novel amides of 1,1-bis-(carboxymethylthio)-1-arylethanes derivatives showed good inhibitory action against acetylcholinesterase (AChE) butyrylcholinesterase (BChE), and human carbonic anhydrase I and II isoforms (hCA I and II). AChE inhibitors, interacting with the enzyme as their primary target, are applied as relevant drugs and toxins. Many clinically established drugs are carbonic anhydrase inhibitors, and it is highly anticipated that many more will eventually find their way into the market. The novel synthesized compounds inhibited AChE and BChE with K values in the range of 0.64-1.47 nM and 9.11-48.12 nM, respectively. On the other hand, hCA I and II were effectively inhibited by these compounds, with K values between 63.27-132.34 and of 29.63-127.31 nM, respectively.