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 >Synthesis of new 4-(2,5-dimethylpyrrol-l-yl)/4-pyrro1-1-yl Benzoic' and hydrazide analogs and some derived oxadiazole, triazole and pyrrole ring systems: a novel class of potential antibacterial, antifungal and antitubercular agents
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Synthesis of new 4-(2,5-dimethylpyrrol-l-yl)/4-pyrro1-1-yl Benzoic' and hydrazide analogs and some derived oxadiazole, triazole and pyrrole ring systems: a novel class of potential antibacterial, antifungal and antitubercular agents

机译:合成新的4-(2,5-二甲基吡咯-1-基)/ 4-吡咯-1-基苯并肼类似物和一些衍生的恶二唑,三唑和吡咯环系统:一类新型的潜在抗菌,抗真菌和抗结核药代理商

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摘要

A series of 4-(2,5-dimethylpyrrol-l-yl)/4-pyr-rol-l-yl benzoic acid hydrazide analogs, some derived 1,3,4-oxadiazoles, 5-substituted-4-amino-1,2,4-triazolin-3-thione and 2,5-dimethyl pyrroles have been synthesized in good yields and structures of these compounds were established by IR, 'H NMR, 13C NMR, Mass spectral and elemental analysis. These compounds were evaluated for their preliminary in vitro antibacterial, antifungal and antitubercular activities against Mycobacterium tuberculosis H37RV strain by broth dilution assay method. Twelve of these compounds displayed good antimicrobial activity, with a minimum inhibitory concentration (MIC) values l-4ugmL~'. Several compounds 4, 8d, 9, 12c-d and 12f-h exhibited good in vitro antitubercular activity with MIC values 1-2 u.g mL~'. Further, some title compounds were also assessed for their cytotoxic activity (IC50) against mammalian Vero cell lines and A549 (lung adenocarci-noma) cell lines using MTT assay method. The results reveal that these compounds exhibit antitubercular activity at non-cytotoxic concentrations.
机译:一系列的4-(2,5-二甲基吡咯-1-基)/ 4-吡咯--1-基苯甲酸酰肼类似物,一些衍生的1,3,4-恶二唑,5-取代的4-氨基-1合成了高产率的1,2,4-三唑啉-3-硫酮和2,5-二甲基吡咯,并通过IR,1 H NMR,13 C NMR,质谱和元素分析确定了这些化合物的结构。通过肉汤稀释法评估这些化合物对结核分枝杆菌H37RV菌株的初步体外抗菌,抗真菌和抗结核活性。这些化合物中的十二个显示出良好的抗菌活性,最小抑菌浓度(MIC)值为1-4ugmL。几种化合物4、8d,9、12c-d和12f-h表现出良好的体外抗结核活性,MIC值为1-2μg/ mL。此外,还使用MTT测定法评估了一些标题化合物对哺乳动物Vero细胞系和A549(肺腺癌-瘤)细胞系的细胞毒活性(IC50)。结果表明,这些化合物在非细胞毒性浓度下具有抗结核活性。

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