Synthesis and biological evaluation of novel benzothiazole clubbed fluoroquinolone derivatives

被引:36
|
作者
Sharma, Prabodh Chander [1 ]
Kumar, Ravinder [1 ]
Chaudhary, Monika [1 ]
Sharma, Archana [1 ]
Rajak, Harish [2 ]
机构
[1] Kurukshetra Univ, Inst Pharmaceut Sci, Kurukshetra 136119, Haryana, India
[2] Guru Ghasidas Univ, Inst Pharmaceut Sci, Bilaspur, India
关键词
Fluoroquinolones; benzothiazoles; anti-bacterial; analgesic; anthelmintic; POTENTIAL ANTITUMOR AGENTS; ANTIBACTERIAL ACTIVITY; ACID-DERIVATIVES; ANTIMYCOBACTERIAL ACTIVITIES; ANTIMICROBIAL AGENTS; DNA GYRASE; ACCUMULATION; INHIBITION; QUINOLONES; ANALOGS;
D O I
10.3109/14756366.2011.611943
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In the present investigation, synthesis and anti-bacterial, analgesic and anthelmintic evaluation of a novel series of fluoroquinolone derivatives clubbed with benzothiazole moeity has been described. The synthesized compounds were characterised by spectral analysis (IR and H-1 NMR). Preliminary results indicated that the most of the synthesized compounds demonstrated good activities against gram negative and gram positive bacterial strains. Compounds 5a, 5b, 5f and 5k demonstrated potent anti-bacterial activities. Compound 5a exhibited most potent anti-bacterial activity with MIC values of 04, 03, 08 and 15 mu g/mL against B. subtilis, S. aureus, E. coli and P. aeruginosa. Analogs 5a, 5c, 5g and 5h showed promising anthelmintic activity against Eisemia foetida in a low concentration as compared to standard drug piperazine citrate with mean paralysis time ranging 22.60 +/- 2.46 to 31.60 +/- 3.07 min. All synthesized compounds depicted good in vivo analgesic activity with compound 5a exhibiting the most potent activity of 55.19% inhibition of writhing in comparison to the standard drug.
引用
收藏
页码:1 / 10
页数:10
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