Department of Pharmaceutical Sciences, M.D University, Rohtak, Haryana 124001, India.
Pioneer Pharmacy Degree College, Vadodara, Gujarat, India.
Anticancer Agents Med Chem. 2018;18(15):2193-2205. doi: 10.2174/1871520618666180830152701.
Microbial infections have been the major cause of morbidity and mortality for the centuries and continue to present the formidable challenge to the human health. Several studies have been performed to explore the antimicrobial potential of various synthesized chalcone derivatives. The morpholine derivatives are also gaining considerable importance due to diverse biological activities. Hybridization of morpholine and chalcone moiety together can be the useful approach for the development of new effective antimicrobial agents.
A new series of morpholine based heterocyclic diazenyl chalcones (MD1-MD21) was synthesized, characterized and evaluated for antimicrobial potential by tube dilution and agar diffusion methods. The most active derivatives were also evaluated for cytotoxicity towards mouse fibroblast cell line (L929) and the human lung cancer cell line (A549) and for haemolysis to check the toxicity on human red blood cells.
MD-6 was found highly active against different microbial strains, particularly and having the MIC in the range of 1.95 µg/ml to 3.91 µg/ml. MD-9 and MD-21 were also found to have good antimicrobial activity. The most active diazenyl derivatives exhibited very low cytotoxicity towards L929 cell line (IC ranges from 360 µg/ml - 902.3 µg/ml) and A549 cell line (IC ranges from 35.42 µg/ml - 216.4 µg/ml) as compared to the standard drug 5-FU (IC ranges from 1 µg/ml - 2 μg/ml) against these cell lines. The active derivatives showed haemolysis of 10-15% up to 150 µg/ml concentration.
MD-6, MD-9 and MD-21 were found to be most active antimicrobial agents. These derivatives demonstrated high safety profile by exhibiting very low cytotoxicity and also revealed their safety for human blood cells with haemolysis of 0.2-5.5% at their antimicrobial concentration.
微生物感染是几个世纪以来发病率和死亡率的主要原因，并且继续对人类健康构成巨大挑战。已经进行了几项研究来探索各种合成查尔酮衍生物的抗菌潜力。由于具有多种生物活性，吗啉衍生物也变得越来越重要。将吗啉和查尔酮部分杂化在一起可能是开发新的有效抗菌剂的有用方法。
合成、表征并通过管稀释和琼脂扩散法评估了一系列新的基于吗啉的杂环重氮查尔酮（MD1-MD21）的抗菌潜力。还评估了最有效的衍生物对小鼠成纤维细胞系（L929）和人肺癌细胞系（A549）的细胞毒性以及对人红细胞的溶血作用，以检查其对人红细胞的毒性。
MD-6 对不同的微生物菌株表现出高度的活性，特别是 和 的 MIC 在 1.95 µg/ml 至 3.91 µg/ml 的范围内。MD-9 和 MD-21 也表现出良好的抗菌活性。最有效的重氮衍生物对 L929 细胞系（IC 范围为 360 µg/ml - 902.3 µg/ml）和 A549 细胞系（IC 范围为 35.42 µg/ml - 216.4 µg/ml）的细胞毒性非常低，与标准药物 5-FU（IC 范围为 1 µg/ml - 2 µg/ml）相比，对这些细胞系的细胞毒性。活性衍生物在 150 µg/ml 浓度下的溶血率为 10-15%。
MD-6、MD-9 和 MD-21 被发现是最有效的抗菌剂。这些衍生物表现出非常低的细胞毒性，显示出高安全性，并且在其抗菌浓度下对人血红细胞的溶血率为 0.2-5.5%，表明安全性良好。
