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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 >Docking, synthesis, and pharmacological investigation of novel substituted thiazole derivatives as non-carboxylic, anti-inflammatory, and analgesic agents
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Docking, synthesis, and pharmacological investigation of novel substituted thiazole derivatives as non-carboxylic, anti-inflammatory, and analgesic agents

机译：新型取代噻唑衍生物作为非羧酸，抗炎和镇痛剂的对接，合成和药理研究

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摘要

A series of substituted thiazole derivatives (6-16) were synthesized to obtain new compounds with potential anti-inflammatory and analgesic activities. At equimolar oral doses, compounds 3-(piperidin-l-yl-methyl)-l, 3, 4-oxa-diazol-2-thione (14), 5-amino-4-ethyl ester pyrazole (15), and 5-amino-3-phenylpyrazole derivatives (16) displayed anti-inflammatory and analgesic activities significant to those of diclofenac sodium in the carrageenan-induced paw edema test in rat and acetic acid-induced writhing test in mice,-respectively. The most active members of the series (9,11,14, 15, and 16) were selected for ulcerogenic potential study. These compounds exhibited quite less ulcerogenic index in the range of 0.44 to 0.62 whereas diclofenac sodium showed 4.67. The docking study results also indicated that the compound 6,7,8,11, and 14 exhibited the docking score ranging from -3.951 to -4.691.
机译：合成了一系列取代的噻唑衍生物（6-16），以获得具有潜在抗炎和镇痛活性的新化合物。在等摩尔的口服剂量下，化合物3-（哌啶-1-基-甲基）-1、3、4-氧杂二唑-2-硫酮（14），5-氨基-4-乙酯吡唑（15）和5 -氨基-3-苯基吡唑衍生物（16）在大鼠角叉菜胶诱发的爪水肿试验和小鼠乙酸诱发的扭体试验中分别显示出与双氯芬酸钠显着的抗炎和镇痛活性。选择该系列中最活跃的成员（9、11、14、15和16）进行潜在致溃疡性研究。这些化合物在0.44至0.62的范围内表现出相当低的致溃疡指数，而双氯芬酸钠显示为4.67。对接研究结果还表明，化合物6,7,8,11和14的对接得分范围为-3.951至-4.691。

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