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Synthesis, Bioactivity and Molecular Modeling Studies on Potential anti-Alzheimer Piperidinehydrazide-Hydrazones

Synthesis, Bioactivity and Molecular Modeling Studies on Potential anti-Alzheimer Piperidinehydrazide-Hydrazones

Sulunay Parlar, Gozde Sayar, Ayse Hande Tarikogullari, Sumru Sozer Karadagli, Vildan Alptuzun, Ercin Erciyas, Ulrike Holzgrabe

Bioorg Chem. 2019 Jun;87:888-900.

PMID: 30538051

Abstract:

A group of N-benzylpiperidine-3/4-carbohydrazide-hydrazones were designed, synthesized and evaluated for acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) activities, Aβ42 self-aggregation inhibitory potentials, and antioxidant capacities, in vitro. All of the compounds displayed eeAChE and huAChE inhibitory activity in a range of IC50 = 5.68-11.35 µM and IC50 = 8.80-74.40 µM, respectively and most of the compounds exhibited good to moderate inhibitory activity on BuChE enzyme. Kinetic analysis and molecular modeling studies were also performed for the most potent compounds (1g and 1j). Not only the molecular modeling studies but also the kinetic analysis suggested that these compounds might be able to interact with the catalytic active site (CAS) and the peripheral anionic site (PAS) of the enzymes. In the light of the results, compound 1g and compound 1j may be suggested as lead compounds for multifunctional therapy of AD.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP2390547	Thioflavin T - CAS 2390-54-7		2390-54-7	Price

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