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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Piroxicam sulfonates biology-oriented drug synthesis (BIODS), characterization and anti-nociceptive screening
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Piroxicam sulfonates biology-oriented drug synthesis (BIODS), characterization and anti-nociceptive screening

机译:吡罗昔康磺酸盐面向生物学的药物合成(BIODS),表征和抗伤害感受性筛选

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摘要

The present study was designed to synthesize aryl/alkyl sulfonyl substituted derivatives of piroxicam. The structures were elucidated through various spectroscopic procedures like H-1-NMR, C-13-NMR, MS, IR, UV and elemental analysis. The synthesized derivatives (I VI) were screened for anti-nociceptive activity in BALB-c mice by dividing them in five groups (n = 6) for each compound. Test compounds significantly reduced the number of writhes in acetic acid test for peripheral analgesia, but no effect was observed in hot plate test for central analgesia. The compounds possessed good peripheral analgesic effect but no central effect. These compounds were also assessed for acute toxicity in different doses at 50, 100 and 150 mg/kg i.p., and no mortality was observed in animals. In conclusion, the piroxicam derivatives exhibited marked peripheral anti-nociceptive effect with considerable safety.
机译:本研究旨在合成吡罗昔康的芳基/烷基磺酰基取代的衍生物。通过各种光谱学方法(例如H-1-NMR,C-13-NMR,MS,IR,UV和元素分析)阐明了结构。通过将合成的衍生物(I VI)分为每种化合物五个组(n = 6),以筛选BALB-c小鼠的抗伤害感受活性。在进行外周镇痛的乙酸试验中,试验化合物显着减少了扭动次数,但在中枢镇痛的热板试验中未观察到效果。该化合物具有良好的外周镇痛作用,但没有中枢作用。还以50、100和150mg / kg i.p.的剂量评估了这些化合物的急性毒性,在动物中未观察到死亡。总之,吡罗昔康衍生物具有显着的外周抗伤害感受作用,具有相当大的安全性。

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