抗菌剂
化学
对接(动物)
立体化学
金黄色葡萄球菌
肉汤微量稀释
亚胺
青霉素
席夫碱
组合化学
抗菌活性
最小抑制浓度
抗生素
细菌
有机化学
生物化学
生物
护理部
催化作用
医学
遗传学
标识
DOI:10.21271/zjpas.33.2.4
摘要
Four membered cyclic amides that are a broadly utilized class of antimicrobial agents up to now. Moreover, Symmetrical Bis-Schiff bases constitute an extraordinary class of strained compounds with varied applications and building blocks for the synthesis of 2-Azetidinones antibiotics. Because of those over biological significance, this study concludes a versatile synthetic precursor for the synthesis of the new Symmetrical Bis-Schiff bases and 2-Azetidinones in an exceedingly high yield. 2-Azetidinones were synthesized through [2+2] dichloroketene-imine cycloaddition reaction. The structures of the synthesized compounds were characterized by FT-IR, 1H-NMR, and 13C-NMR. Additionally, the products were assayed against two antibacterial types Gram-positive (S. aureus) and Gram-negative (E. coli) microorganisms and two varieties of fungal strains A. niger, T. mentagrophytes by broth microdilution method. As a result, all synthesized compounds displayed good antimicrobial activities against resistant strains. Finally, molecular docking studies were explained the inhibitory activities for the new products with the target (PDB ID: 1MWU) methicillin acyl-Penicillin binding protein 2a from methicillin-resistant Staphylococcus aureus strain 27r at 2.60 Å resolution.
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