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.
One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues / Bais, J., Benedetti, F., Berti, F., Cerminara, I., Drioli, S., Funicello, M., Regini, G., Vidali, M., Felluga, F.. - In: MOLECULES. - ISSN 1420-3049. - ELETTRONICO. - 25:(2020), pp. 18.4152-18.4167. [10.3390/molecules25184152]
One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues
Fabio Benedetti;Federico Berti;Sara Drioli;Maria Funicello;Giorgia Regini;Mattia Vidali;Fulvia Felluga
2020-01-01
Abstract
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.| File | Dimensione | Formato | |
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