In-silico, in-vitro antibacterial activity and toxicity profile of new quinoline derivatives

被引:0
作者
Sambavekar, P. P. [1 ]
Aitawade, M. M. [1 ]
Patil, D. R. [2 ]
Kolekar, G. B. [2 ]
Deshmukh, M. B. [2 ]
Anbhule, P. V. [2 ]
机构
[1] Shivaji Univ, Dept Agrochem & Pest Management, Kolhapur 416004, Maharashtra, India
[2] Shivaji Univ, Dept Chem, Kolhapur 416004, Maharashtra, India
来源
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY | 2013年 / 52卷 / 12期
关键词
Quinoline derivatives; PASS; Antibacterial activity; Staphylococcus aureus; Escherichia coli; Brine shrimp; BIOLOGICAL-ACTIVITY; INHIBITORS; ANALOGS;
D O I
暂无
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The new substituted quinoline derivatives have been synthesized and characterized by various spectroscopic techniques. A prediction of activity spectra for substances (PASS) of synthesized quinoline compounds showed their probabilities of being active for the antibacterial activities. Therefore, all the newly synthesized compounds have been evaluated for their in-vitro antibacterial activity against Staphylococcus aureus and Escherichia coli. It has been observed that 6-chloro-4-phenylquinoline-2,3-dicarboxylic acid 4a selectively active against Gram (-)ve E. coli and 8-chloro-10-phenyl-2,3-dihydropyridazino[4,5-b]quinoline-1,4-dione 5a showed selectivity against Gram (+)ve S. aureus. PASS prediction study indicates that the compound 5a as a potential candidate with a Pa 0.671, maximum from the series. According to the results obtained from brine shrimp (Artemia sauna) lethality bioassay the compounds prove to be non toxic. The computer aided results are in good agreement with experimental results.
引用
收藏
页码:1521 / 1526
页数:6
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