首页> 美国卫生研究院文献>Advanced Pharmaceutical Bulletin >Microwave Assisted Synthesis of 1-5-(Substituted Aryl)-1H-Pyrazol-3-yl-35-Diphenyl-1H-124-Triazole as Antinociceptive and Antimicrobial Agents
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Microwave Assisted Synthesis of 1-5-(Substituted Aryl)-1H-Pyrazol-3-yl-35-Diphenyl-1H-124-Triazole as Antinociceptive and Antimicrobial Agents

机译:微波辅助合成1- 5-(取代芳基)-1H-吡唑-3-基 -35-二苯基-1H-124-三唑作为抗伤害药和抗菌剂

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摘要

>Purpose: An efficient technique has been developed for microwave assisted synthesis of 1-[5-(substituted aryl)-1H-pyrazol-3-yl]-3,5-diphenyl-1H-1,2,4-triazole as antinociceptive and antimicrobial agents.>Methods: The desired compounds (S1-S10) were synthesized by the microwave irradiation via cyclization of formerly synthesized chalcones of 3,5-diphenyl-1H-1,2,4-triazole and hydrazine hydrate in mild acidic condition. All newly synthesized compounds were subjected to study their antinociceptive and antimicrobial activity. The analgesic potential of compounds was tested by acetic acid induced writhing response and hot plate method. The MIC values for antimicrobial activity were premeditated by liquid broth method.>Results: The compounds S1, S2, S4, S6 and S10 were found to be excellent peripherally acting analgesic agents when tested on mice by acetic acid induced writhing method and compounds S3, S6 and S1 at dose level of 100 mg/kg were exhibited superior centrally acting antinociceptive activity when tested by Eddy’s hot plate method. In antimicrobial activity compound S10 found to be broad spectrum antibacterial agent at MIC value of 15.62 µg/ml and compound S6 was exhibited antifungal potential at 15.62 µg/mL on both fungal strains.>Conclusion: Some novel pyrazoles clubbed with 1,2,4-triazole derivatives were synthesized and evaluated as possible antimicrobial, centrally and peripherally acting analgesics.
机译:>目的:已开发出一种有效的技术,用于微波辅助合成1- [5-(取代的芳基)-1H-吡唑-3-基] -3,5-二苯基-1H-1,2 ,4-三唑作为抗伤害药和抗菌剂。>方法:通过微波辐照,将先前合成的3,5-二苯基-1H-1查耳酮环合,合成所需化合物(S1-S10), 2,4-三唑和肼水合物在弱酸性条件下。对所有新合成的化合物进行了抗伤害感受和抗菌活性的研究。通过乙酸诱导的扭体反应和热板法测试化合物的镇痛潜力。 >结果::当用乙酸诱导的小鼠对化合物S1,S2,S4,S6和S10进行镇痛时,发现化合物S1,S2,S4,S6和S10是优良的外周镇痛药。当通过涡流热板法测试时,扭旋方法和剂量为100 mg / kg的化合物S3,S6和S1具有优异的中枢镇痛作用。在抗菌活性中,化合物S10在MIC值为15.62 µg / ml时是广谱抗菌剂,化合物S6在两种真菌菌株中均表现出15.62 µg / mL的抗真菌潜力。>结论:合成了1,2,4-三唑衍生物,并对其可能的抗菌作用,中枢和外周镇痛药进行了评估。

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