Synthesis, Antimicrobial Capability and Molecular Docking of Heterocyclic Scaffolds Clubbed by 2-Azetidinone, Thiazole and Quinoline Derivatives

化学 噻唑 喹啉 抗菌剂 连接器 组合化学 分子 大肠杆菌 对接(动物) 立体化学 生物化学 有机化学 操作系统 医学 护理部 计算机科学 基因
作者
Nisheeth C. Desai,J P Harsora,Jahnvi D. Monapara,Vijay M. Khedkar
出处
期刊:Polycyclic Aromatic Compounds [Taylor & Francis]
卷期号:42 (7): 3924-3938 被引量:18
标识
DOI:10.1080/10406638.2021.1877747
摘要

A new set of molecules was designed and synthesized by compilation of pharmacologically potential segments thiazole and quinoline bridged by 2-azetidinone as a linker in a single molecular skeleton. Structural analysis of synthesized molecules (5a-p) was executed by IR, 1H NMR, 13C NMR, and mass spectroscopy techniques. Aforesaid compounds were analyzed for investigation of their antimicrobial capability against several bacterial and fungal strains. The synthesized compounds 5b, 5f, 5h, 5i, 5k, and 5l were active against bacterial strains while compounds 5j and 5k were active against fungal strains. Synthesized compounds were found to be potential inhibitors against gram-negative bacterial strains Escherichia coli and Pseudomonas aeruginosa, while the same were not effective against gram-positive strains of Staphylococcus aureus and Streptococcus pyogenes. Compounds with electron-releasing substituents were active molecules against all fungal strains used in screening. Also, the influence of substituents on the antimicrobial activity of target molecules (5a-p) was discussed. Molecular docking study against crucial microbial target β-Ketoacyl-acyl carrier protein (ACP) synthase III (FabH) could provide valuable insights into their plausible mechanism of action.
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