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Design, characterization, computational studies, and pharmacological evaluation of substituted- N′ -[(1E) substituted-phenylmethylidene]benzohydrazide analogs
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2012-10-19 , DOI: 10.1007/s00044-012-0270-0 Suman Bala , Goldie Uppal , Sunil Kamboj , Vipin Saini , D. N. Prasad
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2012-10-19 , DOI: 10.1007/s00044-012-0270-0 Suman Bala , Goldie Uppal , Sunil Kamboj , Vipin Saini , D. N. Prasad
A series of substituted-N′-[(1E)-substituted-phenylmethylidene]benzohydrazide analogs were synthesized and authenticated by TLC, UV–Visible, FTIR, and NMR spectroscopic techniques. The physicochemical similarity of the new analogs with standard drugs was assessed by calculating from a set of ten physicochemical properties using software programs. The information so obtained can be related to prediction of biological activity for important targets. All the target compounds 4a–n were evaluated for their antioxidant, anti-inflammatory, and antimicrobial activity using different in vitro models. The test compounds demonstrated good similarity values with respect to the standard drugs. The compounds 4c, 4d, and 4e have emerged as important lead compounds showing potential anti-inflammatory; and 4b, 4f, and 4c having antioxidant profile. While studying MIC against bacterial strains 4c, 4f, 4i, 4k, and 4m were most active among all the target compounds. All compounds were found to have very good antifungal activity. The compounds having nitro substitution at the arylidene moiety i.e., 4c and 4f showed the most potent antifungal as well as antibacterial activities. While studying total antioxidant activity, all target compounds were found to have good antioxidant activity.
中文翻译:
设计,表征,计算研究和药理学评估的取代-N'-[((1E)取代-苯亚甲基]苯并肼类似物
通过TLC,UV-Visible,FTIR和NMR光谱技术合成并鉴定了一系列取代的N' -[[(1E)-取代的苯基亚甲基]苯并肼类似物。通过使用软件程序从一组十个物理化学性质中进行计算,评估了新类似物与标准药物的物理化学相似性。如此获得的信息可以与重要靶标的生物活性预测有关。使用不同的体外模型评估了所有目标化合物4a – n的抗氧化,抗炎和抗菌活性。测试化合物相对于标准药物显示出良好的相似性值。化合物4c,4d和4e已作为重要的先导化合物出现,显示出潜在的抗炎作用;和图4b,图4F和图4c具有抗氧化轮廓。在研究针对细菌菌株4c,4f,4i,4k和4m的MIC时,在所有目标化合物中活性最高。发现所有化合物都具有非常好的抗真菌活性。在亚芳基部分即4c和4f具有硝基取代的化合物显示出最有效的抗真菌和抗菌活性。在研究总抗氧化剂活性时,发现所有目标化合物均具有良好的抗氧化剂活性。
更新日期:2012-10-19
中文翻译:
设计,表征,计算研究和药理学评估的取代-N'-[((1E)取代-苯亚甲基]苯并肼类似物
通过TLC,UV-Visible,FTIR和NMR光谱技术合成并鉴定了一系列取代的N' -[[(1E)-取代的苯基亚甲基]苯并肼类似物。通过使用软件程序从一组十个物理化学性质中进行计算,评估了新类似物与标准药物的物理化学相似性。如此获得的信息可以与重要靶标的生物活性预测有关。使用不同的体外模型评估了所有目标化合物4a – n的抗氧化,抗炎和抗菌活性。测试化合物相对于标准药物显示出良好的相似性值。化合物4c,4d和4e已作为重要的先导化合物出现,显示出潜在的抗炎作用;和图4b,图4F和图4c具有抗氧化轮廓。在研究针对细菌菌株4c,4f,4i,4k和4m的MIC时,在所有目标化合物中活性最高。发现所有化合物都具有非常好的抗真菌活性。在亚芳基部分即4c和4f具有硝基取代的化合物显示出最有效的抗真菌和抗菌活性。在研究总抗氧化剂活性时,发现所有目标化合物均具有良好的抗氧化剂活性。