Gawdzik Barbara, Kowalczyk Paweł, Koszelewski Dominik, Brodzka Anna, Masternak Joanna, Kramkowski Karol, Wypych Aleksandra, Ostaszewski Ryszard
Institute of Chemistry, Jan Kochanowski University, Uniwersytecka 7, 25-406 Kielce, Poland.
Department of Animal Nutrition, The Kielanowski Institute of Animal Physiology and Nutrition, Polish Academy of Sciences, Instytucka 3, 05-110 Jabłonna, Poland.
Membranes (Basel). 2022 Feb 18;12(2):238. doi: 10.3390/membranes12020238.
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 strains. We tested 16 newly synthesized DHPMs as antimicrobial agents on model 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 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.
在此，我们展示了在无溶剂条件下由氯化铵催化的Biginelli反应制得的3,4-二氢嘧啶-2(1H)-酮（DHPMs）的生物学研究。到目前为止，尚未对DHPMs针对致病菌株的生物活性进行测试。我们在模型菌株（K12和R2 - R4）上测试了16种新合成的DHPMs作为抗菌剂。使用MIC和MBC测试以及对细菌DNA进行修饰后Fpg的消化进行的初步细胞研究表明，这些化合物作为抗菌剂可能比常用抗生素（如环丙沙星（ci）、博来霉素（b）和氯唑西林（cl））具有更大的潜力。基于所使用的模型菌株，所描述的化合物对致病菌株具有高度特异性，并且在大流行时代可能会在未来作为临床和医院感染中常用抗生素的新替代品。
