Synthesis of some 2-azitidinones (β-lactams) as antibiotic mimics and screening of their antimicrobial activity

Kamrunnahar Happy, Sumaiya Khan, Umme Aiman Liza, Afsana Mimi, Md Rafikul Islam, Mohammad Mamun Hossain
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Abstract

2-Azetidinones (β-lactams) possess broad and potent bioactivity owing to the presence of lactam rings. As evidence has shown, it is one of the most critical biological frameworks. Some new 2- azetidinones have been synthesized from corresponding Schiff bases using different amines and aldehydes. All compounds (Schiff bases and β- lactams) were synthesized for comparison research using conventional and microwave techniques. The microwave approach has been found to reduce reaction time and boost yield drastically. Analysis combining elemental (C, H, and N) and spectroscopic approaches (NMR, IR, and UV) have been applied to ensure the Schiff bases constitution and corresponding β-lactams constitution. The newly synthesized compound's antibacterial action was estimated opposite to one gram-positive and one gram-negative bacteria. One compound (A-03) among synthesized 2-azitidinones was shown significant activity against the gram-positive bacteria. The other synthesized compounds had no substantial activity on either of the microorganisms. J. Bangladesh Acad. Sci. 48(1); 111-119: June 2024
作为抗生素模拟物的一些 2-叠氮丁酮(β-内酰胺)的合成及其抗菌活性筛选
由于内酰胺环的存在,2-氮杂环丁酮(β-内酰胺)具有广泛而有效的生物活性。有证据表明,它是最重要的生物框架之一。我们利用不同的胺和醛从相应的希夫碱合成了一些新的 2-氮杂环丁酮。所有化合物(希夫碱和 β-内酰胺)的合成均采用传统和微波技术进行比较研究。研究发现,微波方法可以缩短反应时间并大大提高产量。通过元素分析(C、H 和 N)和光谱分析(核磁共振、红外光谱和紫外光谱),确定了希夫碱的结构和相应的 β-内酰胺的结构。新合成的化合物对一种革兰氏阳性菌和一种革兰氏阴性菌具有抗菌作用。在合成的 2-azitidinones 类化合物中,有一个化合物(A-03)对革兰氏阳性菌具有显著的抗菌活性。其他合成的化合物对这两种微生物都没有实质性的活性。48(1); 111-119: June 2024
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