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One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues.

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.

SUBMITTER: Bais J

PROVIDER: S-EPMC7571164 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature

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One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues.

Bais Jessica J Benedetti Fabio F Berti Federico F Cerminara Iole I Drioli Sara S Funicello Maria M Regini Giorgia G Vidali Mattia M Felluga Fulvia F

Molecules (Basel, Switzerland) 20200910 18

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 IC<sub>50</sub> in the range 100 nM-50 μ ...[more]

PMID: 32927879

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