Bibliographic Details
| Title: |
One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues |
| Authors: |
Jessica Bais, Fabio Benedetti, Federico Berti, Iole Cerminara, Sara Drioli, Maria Funicello, Giorgia Regini, Mattia Vidali, Fulvia Felluga |
| Source: |
Molecules, Vol 25, Iss 18, p 4152 (2020) |
| Publisher Information: |
MDPI AG, 2020. |
| Publication Year: |
2020 |
| Collection: |
LCC:Organic chemistry |
| Subject Terms: |
Alzheimer’s disease, dihydropyrimidinones, Biginelli reaction, β-secretase, BACE-1 inhibitors, Organic chemistry, QD241-441 |
| More Details: |
A library of dihydropyrimidinones was synthesized via a “one-pot” three component Biginelli reaction using different aldehydes in combination with β-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 β-secretase inhibitory activity. The majority of the compounds resulted to be active, with IC50 in the range 100 nM–50 μM. |
| Document Type: |
article |
| File Description: |
electronic resource |
| Language: |
English |
| ISSN: |
1420-3049 |
| Relation: |
https://www.mdpi.com/1420-3049/25/18/4152; https://doaj.org/toc/1420-3049 |
| DOI: |
10.3390/molecules25184152 |
| Access URL: |
https://doaj.org/article/5f43fc193c9c4cd89b8d7d919e79250c |
| Accession Number: |
edsdoj.5f43fc193c9c4cd89b8d7d919e79250c |
| Database: |
Directory of Open Access Journals |
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