The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes

DHPM 作为生物毒性剂对病原菌细菌膜的评价

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作者:Barbara Gawdzik, Paweł Kowalczyk, Dominik Koszelewski, Anna Brodzka, Joanna Masternak, Karol Kramkowski, Aleksandra Wypych, Ryszard Ostaszewski

Abstract

Herein, we present biological studies on 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) obtained via Biginelli reaction catalyzed by NH4Cl under solvent-free conditions. Until now, DHPMs have not been tested for biological activity against pathogenic E. coli strains. We tested 16 newly synthesized DHPMs as antimicrobial agents on model E. coli strains (K12 and R2-R4). Preliminary cellular studies using MIC and MBC tests and digestion of Fpg after modification of bacterial DNA suggest that these compounds may have greater potential as antibacterial agents than typically used antibiotics, such as ciprofloxacin (ci), bleomycin (b) and cloxacillin (cl). The described compounds are highly specific for pathogenic E. coli strains based on the model strains used and may be engaged in the future as new substitutes for commonly used antibiotics in clinical and nosocomial infections in the pandemic era.

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