King Faisal University, College of Science, Department of Chemistry, P. O. Box 400 Al Hufuf, 31982 Al Ahsa, Saudi Arabia.
Mansoura University, Faculty of Science, Department of Chemistry, Mansoura 35516, Egypt.
Eur J Med Chem. 2017 Oct 20;139:107-113. doi: 10.1016/j.ejmech.2017.07.079. Epub 2017 Aug 2.
Two series of fused tricyclic sultams (carboxylates, 3a, b and 5a, f, g and anilides 5b-e) were synthesized from saccharin and their chemical structures were confirmed by spectroscopic tools. Then, their antibacterial activities and MIC were evaluated against two strains of gram positive and gram-negative bacteria. The MIC values of the tested compounds are in the of range 8-33 μg/ml. In addition, their DNA cleavage ability, binding affinity and their anticancer activities against hepatic cancer cell were tested. And their antioxidant activities were also measured. Four carboxylate derivatives (3a, 5a, 5f and 5g) and one anilide (5d) of the tested compounds proved to be the highest activity all over the study.
合成了两组融合的三环磺酰胺（羧酸酯 3a、b 和 5a、f、g 以及酰胺 5b-e），并通过光谱工具确认了它们的化学结构。然后，评估了它们对两种革兰氏阳性和革兰氏阴性细菌的抗菌活性和 MIC。测试化合物的 MIC 值在 8-33μg/ml 范围内。此外，还测试了它们的 DNA 切割能力、结合亲和力以及对肝癌细胞的抗癌活性，并测量了它们的抗氧化活性。在所研究的化合物中，四种羧酸酯衍生物（3a、5a、5f 和 5g）和一种酰胺（5d）被证明具有最高的活性。
