Synthesis, <i>in vitro</i> and docking studies of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one derivatives as agents for the treatment of Alzheimer's disease
نویسندگان
چکیده
Alzheimer's disease is a chronic neurodegenerative disease, which characterized mainly by progressive decrease in intellectual abilities, memory impairment and change person's personality. Unfortunately, there are practically no medicines that act on pathogenesis of disease. The development new highly effective for the treatment this pathology an actual area pharmaceutical research. aim work to search among 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one compounds with anticholinesterase antiamyloid activities. As result, it was found 4d, 4e 4f have high ability, their structure contain residues hydroxy-methoxyphenyl fragments. Structures 4c, 4g, 4h, 4j, 4k, 4m, 4n 4p showed slightly less activity, effect did not differ statistically from Donepezil. Compounds 4e, 4k 4m greatest ability inhibit formation amyloid, comparable GV-971. It should be noted molecular docking data consistent results determination activity studied obtained vitro. Thus, prospects future studies these possibility creating active substance diseases been revealed.
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ژورنال
عنوان ژورنال: Chimica techno acta
سال: 2022
ISSN: ['2411-1414', '2409-5613']
DOI: https://doi.org/10.15826/chimtech.2022.9.2.04