H. Maruthesh, Manjunatha S. Katagi, B.P. Nandeshwarappa
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引用次数: 1
摘要
以1-甲基-2-氧-1,2-二氢喹啉-3-甲醛(1)为原料，与不同取代苯胺(2a-j)在乙醇中缩合，成功合成了一系列(E)-1-甲基-3-(取代苯基)甲基喹啉-2(1H)- 1希夫碱(3a-j)喹啉基团。通过质子(1H)和碳(13C)核磁共振谱、傅里叶变换红外(FT-IR)、质谱研究和元素分析证实了新合成化合物的结构。采用琼脂孔扩散法对革兰氏阳性菌(地衣芽孢杆菌和蜡样芽孢杆菌)、革兰氏阴性菌(大肠杆菌和醋酸杆菌)和黄曲霉和黄曲霉进行了体外抑菌试验。利用微板alamar blue assay (MABA)法对结核分枝杆菌H37Rv菌株进行体外抗结核活性筛选，筛选出具有较好抗结核活性的化合物(3b、3c、3d、3f、3g和3j)，提供了抗结核活性的重要信息。并对合成的化合物的结构活性进行了讨论。化合物3a、3c、3d、3f和3g与不同取代基连接在苯基环上表现出良好的适应性。
A convenient synthesis, characterization and biological evaluation of novel schiff base heterocycles as potential antimicrobial, antitubercular agents and their structural activity relationship
A series of (E)-1-methyl-3-((substituted phenylimino)methyl)quinolin-2(1H)-one schiff bases (3a-j) bearing quinoline moiety synthesized successfully in ethanol by condensation of starting material 1-methyl-2-oxo-1,2-dihydroquinoline-3-carbaldehyde (1) with various substituted anilines (2a-j). The structure of the newly synthesized compounds was confirmed by proton (1H) and carbon (13C) nuclear magnetic resonance spectroscopy, Fourier transformation infrared (FT-IR), Mass spectroscopic study and elemental analysis. The in-vitro antimicrobial activity of the synthesized compounds was undertaken by agar well diffusion method against gram positive bacteria (Bacillus licheniformis and Bacillus cereus) gram negative bacteria (Escherichia coli and Acetobactor sp.) and antifungal activity against (Aspergillus Flavus and Pichnanomala). Further the compounds which shows good activity (3b, 3c, 3d, 3f, 3g and 3j) are screened for in-vitro antitubercular activity by Micro-plate alamar blue assay (MABA) method against mycobacterium tuberculosis H37Rv strain provided important information about activity against these strains. The structure activities of the synthesized compounds were also discussed. Compounds 3a, 3c, 3d, 3f and 3g show good argument with the different substituent attached to the phenyl ring.
期刊介绍：
The "Current Chemistry Letters" is a peer-reviewed international journal which aims to publish all the current and outstanding research articles, reviews and letters in chemistry including analytical chemistry, green chemistry, inorganic chemistry, organic chemistry, physical chemistry, etc. This journal is dedicated to serve all academic and industrial researchers and scientists who are expert in all major advances in chemistry research. The journal aims to provide the most complete and reliable source of information on current developments in these fields. The emphasis will be on publishing quality articles rapidly and openly available to researchers worldwide. Please note readers are free to read, download, copy, distribute, print, search, or link to the full texts of articles published on this journal. Current Chemistry Letters is an open access journal, which provides instant access to the full text of research papers without any need for a subscription to the journal where the papers are published. Therefore, anyone has the opportunity to copy, use, redistribute, transmit/display the work publicly and to distribute derivative works, in any sort of digital form for any responsible purpose, subject to appropriate attribution of authorship. Authors who publish their articles may also maintain the copyright of their articles.
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