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Synthesis of thiazole clubbed pyrazole derivatives as apoptosis inducers and anti-infective agents
Materials Today Chemistry ( IF 6.7 ) Pub Date : 2020-09-01 , DOI: 10.1016/j.mtchem.2020.100335
K.K. Bansal , J.K. Bhardwaj , P. Saraf , V.K. Thakur , P.C. Sharma

Abstract Fourteen N-[{(substituted-phenylthiazol-2-yl)-3-aryl-1H-pyrazol-4-yl}methylene]-5-substituted-thiazol-2-amine (5a-n) analogs were synthesized by the reaction of 3-aryl-1-(thiazol-2-yl)-1H-pyrazole-4-carbaldehyde and substituted thiazole amines. The structures of prepared compounds were delineated by elemental analysis, FT-IR and 1H NMR spectra. These analogs were scrutinized for in vitro anti-infective and cytotoxic activities. Some thaizole clubbed pyrazole derivatives were assessed for their cytological changes in germ cells of Capra hircus by using histomorphological analysis, fluorescence assay and apoptosis quantification. Compound 5l having 4-NO2 substituent induced the significant apoptosis in tested cells of Capra hircus. The results revealed that compounds 5c, 5e, 5k, and 5l have commendable antibacterial activity within MIC range of 62.5–250 μg/ml. Compound 5c emerged as a potent antimalarial compound by exhibiting IC50 value of 0.23 μg/ml and compound 5j induced paralysis of Pherentima posthuma at 8.6 ± 1.94 min and death at 20 ± 5.04 min, respectively. Compound 5j revealed an excellent cytotoxicity at IC50 value of 30.7 and

中文翻译:

作为细胞凋亡诱导剂和抗感染剂的噻唑棒状吡唑衍生物的合成

摘要 14 个 N-[{(取代-苯基噻唑-2-基)-3-芳基-1H-吡唑-4-基}亚甲基]-5-取代-噻唑-2-胺 (5a-n) 类似物通过以下方法合成: 3-芳基-1-(噻唑-2-基)-1H-吡唑-4-甲醛和取代的噻唑胺的反应。通过元素分析、FT-IR和1H NMR光谱描绘了所制备化合物的结构。仔细检查这些类似物的体外抗感染和细胞毒性活性。通过使用组织形态学分析、荧光测定和细胞凋亡定量,评估了一些噻唑棒状吡唑衍生物在 Capra hircus 生殖细胞中的细胞学变化。具有4-NO 2 取代基的化合物5l在被测试的Capra hircus细胞中诱导显着的细胞凋亡。结果表明,化合物 5c、5e、5k、和 5l 在 62.5-250 μg/ml 的 MIC 范围内具有值得称赞的抗菌活性。化合物 5c 作为有效的抗疟化合物出现,IC50 值为 0.23 μg/ml,化合物 5j 分别在 8.6 ± 1.94 分钟和 20 ± 5.04 分钟时诱导 Pherentima posthuma 麻痹和死亡。化合物 5j 在 IC50 值为 30.7 时显示出优异的细胞毒性,并且
更新日期:2020-09-01
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