黄酮类似物的抗菌活性

Kamlesh Kn, Sivakumar T, Afroze A
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引用次数: 7

摘要

背景:大多数现有抗菌药物已产生耐药性;有些药物有严重的毒性和副作用。因此,有必要发现新的化合物,不仅要有效,而且要毒性更小,成本更低。目的:本研究的目的是开发新的合成抗菌药物(抗菌和抗真菌),如3-取代黄酮/黄烷酮衍生物,这应该是有效的,低毒。方法:尝试合成一系列新的3-甲基黄酮衍生物,并合成一系列3-羟基黄酮类似物。通过紫外、红外、H-NMR1、C-NMR13和质谱等手段对化合物的结构进行了分析和鉴定。采用杯盘法对合成的化合物进行体外抗菌筛选,确定抑制区。结果:合成了3-甲基黄酮和3-羟基黄酮衍生物两个系列(各10个)。用各种光谱方法对化合物的结构进行了表征和确定。合成的化合物对3-革兰氏阳性、3-革兰氏阴性和2-革兰氏真菌的体外抑菌活性进行了筛选。结论:部分3-羟基黄酮衍生物(1b、3b、4b和5b)和3-甲基黄酮衍生物(3a、1a、2a和4a)具有较强的抗菌活性。研究发现,3-羟基黄酮衍生物对革兰氏阴性菌活性最强,而3-甲基黄酮衍生物对革兰氏阳性菌活性最强。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Antimicrobial Activity of Flavone Analogues
Background: Most of the available antimicrobial drugs have developed resistance; some of them suffer from severe toxicity, side effects. So, there is a need to discover novel compound(s) which should not only be potent, but also less toxic and cost effective. Objectives: The aim of the study is to develop new synthetic antimicrobial agents (Anti-bacterial and anti-fungal) such as 3-substituted flavone/flavanone derivatives, which should be significantly potent with low toxicity. Method: An attempt was made to synthesize a newer series of 3-methyl flavanone derivatives together with the synthesis of a series of 3-hydroxyl flavone analogues. The structures of the test compounds were elucidated and established by UV, IR, H-NMR1, C-NMR13 and mass spectrometry. The synthesized compounds were subjected for in vitro antimicrobial screening using cup plate methods, followed by the determination of zone of inhibitions. Results: Two series (each 10) of 3-methyl flavanone and 3-hydroxy flavone derivatives were synthesized. The structures of the test compounds were characterized and established by various spectroscopic methods. The synthesized compounds were screened for in vitro antibacterial and antifungal activity against different strains (3- Gram positive, 3-Gram negative and 2-fungal strains). Conclusion: Some of the 3-hydroxyl flavones derivatives (1b, 3b, 4b, and 5b) and 3-methyl flavanone derivatives (3a, 1a, 2a and 4a) were found to elicit potent antimicrobial activity. The study revealed that 3-hydroxy flavone derivatives were found to be most active against Gram negative, while 3-methyl flavanone derivatives were active against Gram positive bacteria.
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