A convenient synthesis and biological activity of novel thieno[2,3-c]pyrazole compounds as antimicrobial and anti-inflammatory agents.

Bioorganicheskaia khimiia Pub Date : 2015-01-01
Adel M Kamal El-Dean, Remon M Zaki, Abdullah Y Abdulrazzaq
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Abstract

A new method for synthesizing 4-amino-3-methyl-1-phenyl-1H-5-substituted thieno[2,3-c]pyrazole was reported. The substituted groups at position 5 include carbonitrile, carboxamide, N-phenyl carboxamide, and benzoyl groups. The newly synthesized compounds and their derivatives were characterized by elemental analysis and spectroscopy (IR, 1H NMR, and mass spectra). Furthermore, some of these synthesized compounds were screened against various pathogenic bacterial and fungal strains. The results demonstrate that most of the synthesized compounds possess a significant antibacterial activity against gram-positive and gram-negative bacteria. In addition, most of these compounds showed a remarkable anti-fungal activity. On the other hand, some of the synthesized compounds possess high anti-inflammatory activity, which was demonstrated using the carrageenan-induced rat paw edema assay.

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新型噻吩[2,3-c]吡唑类抗菌抗炎化合物的合成及生物活性研究。
报道了一种合成4-氨基-3-甲基-1-苯基- 1h -5取代噻吩[2,3-c]吡唑的新方法。第5位的取代基包括碳腈、甲酰胺、n -苯基甲酰胺和苯甲酰。新合成的化合物及其衍生物通过元素分析和光谱(IR、1H NMR和质谱)进行了表征。此外,对合成的部分化合物进行了抗多种致病菌和真菌菌株的筛选。结果表明,大多数合成的化合物对革兰氏阳性菌和革兰氏阴性菌均具有显著的抗菌活性。此外,这些化合物大多显示出显著的抗真菌活性。另一方面,一些合成的化合物具有较高的抗炎活性,这在卡拉胶诱导的大鼠足跖水肿实验中得到了证实。
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