Dehydroabietylamine derived bistetrazoles from ultrasound-assisted pseudo-seven-component Ugi reactions act as efficient and selective inhibitors of cholinesterases
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY REPORTS(2024)
摘要
The reaction of dehydroabiethylamine (DHA) with isocyanides and formaldehyde produces varying products depending on the conditions employed. In a 4-component Ugi reaction using benzyl isocyanide, para-formaldehyde, and TMS-azide, the anticipated tetrazole is formed. Nevertheless, other isocyanides were un-successful in these conditions. Upon substituting paraformaldehyde with formalin and utilizing ultrasound instead, bis-tetrazole formation was obtained in a pseudo-7-component reaction. A bis-benzyl-substituted tet-razole 5 demonstrated significant AChE and BChE inhibition in Ellman's assays. Molecular modeling corrobo-rated these results, with compound 5 identified as a mixed-type inhibitor for both enzymes.
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关键词
Dehydroabietylamine,Tetrazoles,Cholinesterases,Inhibition,Ugi reaction
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