期刊
MOLECULES
卷 25, 期 18, 页码 -出版社
MDPI
DOI: 10.3390/molecules25184152
关键词
Alzheimer's disease; dihydropyrimidinones; Biginelli reaction; beta-secretase; BACE-1 inhibitors
资金
- Universita degli Studi di Trieste-Finanziamento di Ateneo per progetti di ricerca scientifica (FRA)
A library of dihydropyrimidinones was synthesized via a one-pot three component Biginelli reaction using different aldehydes in combination with beta-dicarbonyl compounds and urea. Selected 2-thiooxo and 2-imino analogs were also obtained with the Biginelli reaction from thiourea and guanidine hydrochloride, respectively. The products were screened in vitro for their beta-secretase inhibitory activity. The majority of the compounds resulted to be active, with IC50 in the range 100 nM-50 mu M.
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