首页> 外文期刊>Medicinal Chemistry Research >Microwave-assisted synthesis of some new tetrazolo[1,5-a]quinoline-based benzimidazoles catalyzed by p-TsOH and investigation of their antimicrobial activity
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Microwave-assisted synthesis of some new tetrazolo[1,5-a]quinoline-based benzimidazoles catalyzed by p-TsOH and investigation of their antimicrobial activity

机译:p-TsOH催化微波合成一些新的基于四唑[1,5-a]喹啉的苯并咪唑类化合物及其抗菌活性

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摘要

Keeping the objective to build up a new structural class of potent antimicrobials, a series of some new 4-Benzimidazol-2-yl tetrazolo[1,5-a]quinoline derivatives has been synthesized by reaction of tetrazolo[1,5-a]quinoline-4-carbaldehyde and o-phenylenediamine in the presence of an organocatalyst p-TsOH under the influence of microwave irradiation. The identity of all the compounds has been established by 1H NMR, 13C NMR, FTIR, and elemental analysis. The synthesized compounds were subjected to in vitro antimicrobial screening against a representative panel of pathogenic strains including three Gram-positive bacteria (Bacillus subtilis, Clostridium tetani, and Streptococcus pneumoniae) and three Gram-negative bacteria (Escherichia coli, Salmonella typhi, and Vibrio cholerae) as well as two fungal organisms (Aspergillus fumigatus and Candida albicans) by employing broth microdilution method. Of the compounds studied, compound 5e demonstrated significant activity against a Gram-positive bacteria Bacillus subtilis.
机译:为了建立一种新的有效抗菌剂结构类别的目标,通过四唑并[1,5-a]的反应合成了一系列新的4-苄基咪唑-2-基四唑并[1,5-a]喹啉衍生物。有机催化剂p-TsOH存在下,在微波辐射的影响下,喹啉-4-甲醛和邻苯二胺。通过 1 1 H NMR, 13 C NMR,FTIR和元素分析确定了所有化合物的身份。合成的化合物针对代表性的致病菌株进行体外抗菌筛选,所述致病菌株包括三种革兰氏阳性菌(枯草芽孢杆菌,破伤风梭菌和肺炎链球菌)和三种革兰氏阴性菌(大肠杆菌,鼠伤寒沙门氏菌和霍乱弧菌) )和两种真菌(烟曲霉和白色念珠菌)采用肉汤微稀释法。在研究的化合物中,化合物5e表现出对革兰氏阳性细菌枯草芽孢杆菌的显着活性。

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    《Medicinal Chemistry Research》 |2011年第6期|p.782-789|共8页
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