4.6 Article

Design, Synthesis, and In Vitro and In Silico Approaches of Novel Indanone Derivatives as Multifunctional Anti-Alzheimer Agents

Journal

ACS OMEGA
Volume 7, Issue 50, Pages 47378-47404

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acsomega.2c06906

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Funding

  1. Anadolu University Faculty of Pharmacy Central Research Laboratory (MERLAB)

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Alzheimer's disease is a progressive neurological disorder that affects memory and cognitive function in the elderly. This study focused on the chemical structure of donepezil and designed 42 novel derivatives. The compounds D28-D30 and D37-D39 showed promising antioxidant, enzyme inhibition, and plaque inhibition activities, suggesting their potential in treating AD symptoms and providing palliative care.
Alzheimer's disease (AD) is a neurological, progressive illness that typically affects the elderly and is clinically distinguished by memory and cognitive decline. Due to a number of factor s , including the absence of a radical treatment, an increase in the patient population over time, the high cost of care and treatment, and a significant decline in patients' quality of life, the importance of this disease has increased. These factors have all prompted increased interest among researchers in this field. The chemical structure of the donepezi l molecule, the most popular and effective treatment response for AD, served as the basis for the design and synthesis of 42 novel indan-1-one derivatives in this study. Using IR, 1H, and 13C NMR as well as mass spectroscopic techniques, the compounds' structures were identified. Research on the compounds' antioxidant activities, cholinesterase (ChE) enzyme inhibition, monoamine oxidase (MAO) A and B inhibitory activities, beta-amyloid plaque inhibition, and cytotoxicity impact was carried out. Inhibition of beta-amyloid plaque aggregation; effective inhibition of AChE, BChE, and MAO-B enzymes; and significant antioxidant act i v i t y were all demonstrated by compounds D28-D30 and D37-D39. Because of their various actions, it was hypothesized that the related compounds may be usef u l in treating AD symptoms as well as providing palliative care.

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