Acetylcholinesterase inhibitory potencies of new pyrazoline derivatives

Abstract

Alzheimer's disease (AD) has no current cure and its mechanism is not fully known, but treatments for symptoms are available. Acetylcholinesterase (AChE) has been reported to be an applicable therapeutic target in patient with AD. Acetylcholinesterase inhibitors (AChEIs) are commonly used for it. For this purpose, novel series of pyrazoline based compounds [2-(3-(4-methoxyphenyl)-5-aryl-4,5-dihydro-1H-pyrazol-1-yl)benzo[d]thiazole, 1-9] were synthesized and AChE inhibitory potencies were reported here. The results indicated that compound 1 (Ki= 0.13±0.004 μM) possessed the highest AChE inhibitory effect in series, which is two times more potent than the reference compound Tacrin (Ki= 0.26±0.045 μM). So, pyrazoline derivative 1 can be considered as a lead inhibitor in designing new AChE inhibitors.

Total phenolic, total flavonoid contents, and in vitro biological activities of Cephalaria procera

“…Although the pathophysiology of AD has not been clearly established, the cholinergic hypothesis is one of the most accepted causes. According to the cholinergic hypothesis, AD is associated with alterations of cholinergic markers such as cholinesterases (Tuğrak, Gül & Gülçin, 2020;Kahraman et al, 2019). IC 50 values of the extracts were above 200 µg/mL on AChE for all extracts, while IC 50 values for BuChE were determined as below 100 µg/ mL.…”

“…CEP-3 showed more significant tyrosinase inhibitory effects than kojic acid as a positive control (p<0.001) in this study. Studies in the literature show that antioxidant compounds have tyrosinase inhibitory properties (Wang et al, 2018;Morais et al, 2018;Sun, Guo, Zhang & Zhuang, 2017). In this study, we determined that extracts with a high antioxidant effect showed high tyrosinase inhibition.…”

Synthesis, Characterization, Molecular Docking, Acetylcholinesterase and α‐Glycosidase Inhibition Profiles of Nitrogen‐Based Novel Heterocyclic Compounds

“…[19] Currently, some cholinesterase inhibitors (ChEIs) including tacrine, rivastigmine, donepezil, and galantamine are approved for the treatment of AD. [20] It is known that most of these putative ChEIs used today have some side effects including gastrointestinal anomalies, nausea, diarrhea, and hepatotoxicity. It was reported that tacrine, one of these standard clinical inhibitors, had some side effects including nausea, vomiting, stomach upset, weight loss, agitation, diarrhea, shaking, and skin rash.…”

“…So, AChE inhibition has been the most successful and common approach for treatment of AD to date [19] . Currently, some cholinesterase inhibitors (ChEIs) including tacrine, rivastigmine, donepezil, and galantamine are approved for the treatment of AD [20] . It is known that most of these putative ChEIs used today have some side effects including gastrointestinal anomalies, nausea, diarrhea, and hepatotoxicity.…”

Synthesis and some enzyme inhibition effects of isoxazoline and pyrazoline derivatives including benzonorbornene unit

“…[44,45] Currently, some cholinesterase inhibitors including tacrine, rivastigmine, donepezil, and galantamine are approved for the treatment of AD. [46] Both AChE and BChE are the two brain enzymes targeted by these drugs. It is known that most of these putative cholinesterase inhibitors used today have side effects including gastrointestinal anomalies such as nausea, diarrhea, and hepatotoxicity.…”