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synthesis, docking and acetylcholinesterase inhibitory evaluation of 1,3,4-thiadiazole derivatives as potential anti-alzheimer agents
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نویسنده
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mohammadi-farani ahmad ,takesh milad ,mohammadi mahsa ,hosseini amin ,aliabadi amin ,aliabadi alireza
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منبع
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pharmaceutical sciences - 2024 - دوره : 30 - شماره : 3 - صفحه:369 -378
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چکیده
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Background: according to the cholinergic hypothesis for alzheimer’s disease, potentiation of cholinergic neurotransmission is one of the best strategies for combating dementia. methods: a new series of benzamide derivatives bearing 1,3,4-thiadiazole nucleus were synthesized and subsequently, their anticholinesterase activity was evaluated. molecular docking was carried out to explore the likely binding mode and interactions. results: fortunately, some of the tested compounds exhibited more activity than donepezil as a reference drug (ic50 = 0.6 ± 0.05 µm). some of the evaluated derivatives displayed potency in the nanomolar range. compound 7e with fluorine atom on the meta position of the phenyl ring was the most active compound in this series (ic50 = 1.82 ± 0.6 nm). conclusion: the 1,3,4-thiadiazole derivatives that were synthesized and tested in the current manuscript demonstrated remarkable anticholinesterase activity. therefore, these compounds could be suggested as potential anti-alzheimer agents.
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کلیدواژه
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4-thiadiazole ,acetylcholinesterase ,alzheimer disease ,synthesis
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آدرس
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shahrekord university of medical sciences, school of medicine, medical plants research center, basic health sciences institute, department of physiology and pharmacology, iran, kermanshah university of medical sciences, faculty of pharmacy, students research committee, faculty of pharmacy, department of medicinal chemistry, iran, kermanshah university of medical sciences, faculty of pharmacy, pharmaceutical sciences research center, health institute, faculty of pharmacy, department of medicinal chemistry, iran, kermanshah university of medical sciences, faculty of pharmacy, students research committee, faculty of pharmacy, department of medicinal chemistry, iran, shiraz university of medical sciences, school of medicine, department of pharmacology, iran, kermanshah university of medical sciences, faculty of pharmacy, pharmaceutical sciences research center, health institute, faculty of pharmacy, department of medicinal chemistry, iran
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پست الکترونیکی
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aliabadi.alireza@gmail.com
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Authors
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