Abstract
Alzheimer’s disease (AD) is the most common of the degenerative brain diseases and is described together with the impairment of cognitive function. Patients with AD lose the capability to code new memories, and life conditions are extremely difficult. The development of new drugs in this area continues at a great pace. A novel series of thiazole-piperazine hybrids, aimed against Alzheimer’s disease (AD), have been synthesized. The structure identification of synthesized compounds was elucidated by 1HNMR, 13C-NMR, and LCMSMS spectroscopic methods. The inhibitory potential of the synthesized compounds on cholinesterase enzymes was investigated. The compounds 3a, 3c and 3i showed significant inhibitory activity on the acetylcholinesterase (AChE) enzyme. On the other hand, none of the compounds showed significant inhibitory activity on the butyrylcholinesterase (BChE) enzyme. In addition to enzyme inhibition studies, enzyme kinetic studies were performed to observe the effects of the most active inhibitor compounds on the substrate–enzyme relationship. In addition to in vitro tests, docking studies also indicated that compound 3c potentially acts as a dual binding site AChE inhibitor.
Highlights
Alzheimer’s disease (AD) is a condition that rapidly threatens public health, with an increasing number of affected individuals as the world population increases
Results and Discussion piperazin-1-yl)benzaldehyde was synthesized by a reaction of 1-(4-fluorophenyl)piperazine and
Chemistry fluorophenyl)piperazin-1-yl)benzaldehyde was synthesized by a reaction of 1-(4in ethanol with a catalytic amount of CH3 COOH
Summary
Alzheimer’s disease (AD) is a condition that rapidly threatens public health, with an increasing number of affected individuals as the world population increases. AchE inhibitors, inhibitors, including benzylamine biological processes, and they are a significant target in drug design for the treatment of psychiatric and neurological diseases. 2-aminothiazoles the evaluation of monoamine oxidase enzyme inhibitory activity is generally in the treatment of Alzheimer’s disease, the evaluation of monoamine oxidase enzyme inhibitory as anticholinesterase agents. Synthesis of novel preferred withpreferred cholinesterase assays activity is along generally alonginhibition with cholinesterase inhibition assaysthiazole [27,28,29].derivatives bearing a benzylamine moiety and focus on their interested anticholinesterase effects on AChE Based on these these findings, webecame became interestedininthe thebiological biological evaluation.
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