Design, Synthesis and Biological Evaluation of Some New Coumarin Derivatives as Potential Antimicrobial Agents

被引:29
作者
Singh, Lav Kumar [1 ]
Priyanka [1 ]
Singh, Vineeta [2 ]
Katiyar, Diksha [1 ]
机构
[1] Banaras Hindu Univ, Dept Chem, MMV, Varanasi 221005, Uttar Pradesh, India
[2] Cent Drug Res Inst, Div Fermentat Technol, Lucknow 226001, Uttar Pradesh, India
关键词
Coumarins; antibacterial; antifungal; beta-amino alcohol coumarins; log P; GYRASE B; INHIBITORS; RESISTANCE; ALCOHOLS;
D O I
10.2174/1573406410666140902110452
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 4-methyl-7-O-substituted coumarins (3-12) was synthesized and evaluated for in vitro antimicrobial activity against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), four Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and Proteus vulgaris) and three fungal strains (Candida albicans, Cryptococcus terreus and Saccharomyces cerevisiae) by two-fold serial dilution technique. The results of bioactive assay showed that some of the synthesized coumarins displayed comparable or even better antibacterial and antifungal activities against tested strains in comparison with reference drugs erythromycin, novobiocin and amphotericin B. Compound 9 showed potent antimicrobial activities against seven of the nine microbial strains examined in this study with MIC values ranging between 1.09 and 25 mu g/mL and was the most active compound of the series. The present work also describes the effect of substituent on bioactivity.
引用
收藏
页码:128 / 134
页数:7
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