title: Synthesis and biological evaluation of novel benzothiazole clubbed fluoroquinolone derivatives.
abstract: 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 (1)H 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 µg/ 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.
authors: Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, India. sharma_prabodh@rediffmail.com
authors: Prabodh Chander
authors: PC
authors: Sharma
authors: Ravinder
authors: R
authors: Kumar
authors: Monika
authors: M
authors: Chaudhary
authors: Archana
authors: A
authors: Sharma
authors: Harish
authors: H
authors: Rajak
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000871:Anthelmintics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects; D052160:Benzothiazoles / Q000737:chemistry*; D060326:Chemistry Techniques, Synthetic; D004305:Dose-Response Relationship, Drug; D004926:Escherichia coli / Q000187:drug effects; D005260:Female; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D009835:Oligochaeta / Q000187:drug effects; D010879:Piperazines / Q000494:pharmacology; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013055:Spectrophotometry, Infrared; D013211:Staphylococcus aureus / Q000187:drug effects
chemical_list: D000700:Analgesics; D000871:Anthelmintics; D000900:Anti-Bacterial Agents; D052160:Benzothiazoles; D024841:Fluoroquinolones; D010879:Piperazines; C006589:piperazine citrate; C005465:benzothiazole