作为抗菌剂的黄酮类似物。

IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics
K. Naik, Sivakumar Thangavel, A. Alam, Shailendra Kumar
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引用次数: 6

摘要

背景现有的大多数抗菌药物都产生了耐药性,其中一些药物存在严重的毒性和副作用。因此,有必要发现新的化合物,这种化合物不仅应该有效,而且毒性更小,成本效益高。目的本研究的目的是开发新的合成抗菌剂(抗菌和抗真菌),如3-取代黄酮/黄烷酮衍生物,其应具有显著的效力和低毒性。方法尝试合成一系列新的3-甲基黄烷酮衍生物,同时合成一系列3-羟基黄酮类似物。通过紫外光谱、红外光谱、核磁共振氢谱、核磁共振13C-NMR和质谱等方法对试验化合物的结构进行了鉴定和确定。使用杯板法对合成的化合物进行体外抗菌筛选,然后测定抑制区。结果合成了两个系列(每个10个)的3-甲基黄烷酮和3-羟基黄酮衍生物。通过各种光谱方法对测试化合物的结构进行了表征和确定。合成的化合物对不同菌株(3-革兰氏阳性、3-革兰氏阴性和2-真菌菌株)进行了体外抗菌和抗真菌活性筛选。结论发现一些3-羟基黄酮衍生物(1b、3b、4b和5b)和3-甲基黄烷酮衍生物(3a、1a、2a和4a)具有较强的抗菌活性。研究表明,3-羟基黄酮衍生物对革兰氏阴性菌最具活性,而3-甲基黄烷酮衍生物对革兰氏阳性菌最有活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Flavone Analogues as Antimicrobial Agents.
BACKGROUND Most of the available antimicrobial drugs have developed resistance, some of them suffer from severe toxicity and 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, 1H-NMR, 13C-NMR 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. RESULT 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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来源期刊
CiteScore
3.90
自引率
0.00%
发文量
0
期刊介绍: Recent Patents on Inflammation & Allergy Drug Discovery publishes review articles by experts on recent patents in the field of inflammation and allergy drug discovery e.g. on novel bioactive compounds, analogs and targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in inflammation and allergy drug design and discovery.
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