Design, Synthesis, Antimicrobial, and Antioxidant Activities of Novel- {4, 5-(substituted diphenyl)-4H-1, 2, 4-triazol-3-ylthio} Acetyl Chloride
Design, Synthesis, Antimicrobial, and Antioxidant Activities of Novel- {4, 5-(substituted diphenyl)-4H-1, 2, 4-triazol-3-ylthio} Acetyl Chloride
复制标题
新型-{4,5-(取代二苯基)-4H-1,2,4-三唑-3-基硫基}乙酰氯的设计、合成、抗菌和抗氧化活性
DOI：
10.48048/wjst.2018.2178
复制
发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Anurag Khatahar
中科院分区：
文献类型：
--
作者：
Mukesh Kumar;N. Malik;Priyanka Dhiman;P. Verma;Anurag Khatahar
合成了20个具有生物活性的2-{4，5-（取代二苯基）-4H-1，2，4-三唑-3-基硫基}乙酰氯衍生物，研究了它们的抗菌、清除自由基活性。所合成的化合物均通过元素分析和光谱数据进行了表征。以环丙沙星为抗菌药物，氟康唑为抗真菌标准药物，对革兰氏阳性菌：金黄色葡萄球菌MTCC 3160、枯草芽孢杆菌MTCC 441、革兰氏阴性菌：大肠杆菌MTCC 443进行抗菌活性测试，对白色念珠菌MTCC 227和尼日尔MTCC 281进行抗真菌活性测试。与标准药物相比，发现化合物7a 6是最有效的抗菌剂（MIC = 3.12 μg/ml），并且化合物7a 2和7 d1（MIC = 3.12和6.25 μg/ml）对所选菌株具有最有效的抗真菌作用。抗氧化活性研究结果表明，化合物7 b1的抗氧化活性最高，为40.4±0.687 μg/ml，化合物7 b3、7 d 7和7 d4也表现出较好的自由基清除活性。
A series of 20 new biologically active derivatives of 2-{4, 5-(substituted diphenyl)-4H-1,2,4-triazol3-ylthio}acetyl chloride has been synthesized, with the aim to investigate antimicrobial, free radical scavenging activity. All the synthesized compounds were characterized by spectroscopic data and elemental analysis. The final compounds were tested for antibacterial activity against Gram-positive bacteria: Staphylococcus aureus MTCC 3160, Bacillus subtilis MTCC 441; Gram-negative bacteria: Escherichia coli MTCC 443, and, for antifungal activity, against Candida albicans MTCC 227 and Aspergillus niger MTCC 281, taking ciprofloxacin as antibacterial and fluconazole as antifungal standard drugs. Compound 7a6 was found to be the most effective antibacterial (MIC = 3.12 μg/ml), and compounds 7a2 and 7d1 (MIC = 3.12 and 6.25 μg/ml) had the most effective antifungal effects on the selected strains, as compared to the standard drugs. The results of antioxidant studies revealed that compound 7b1 was found to be most active antioxidant, with 40.4±0.687 μg/ml, and compounds 7b3, 7d7, and 7d4 also showed promising free radical scavenging activity, as compared with the standard drug ascorbic acid.