Chemistry Department, Faculty of Arts and Science, Dumlupınar University , Kütahya , Turkey.
J Enzyme Inhib Med Chem. 2013 Oct;28(5):885-93. doi: 10.3109/14756366.2012.692087. Epub 2012 Jul 18.
Xanthene intermediates 4a and 4b were obtained from the reduction of nitro xanthene derivatives 3a and 3b which were synthesized via condensation of dimedone with m-nitrobenzaldehyde and p-nitrobenzaldehyde, respectively. Then xanthene sulfonamide 6a-n, and xanthene carboxamide derivatives 8a-h were synthesized by reaction of amino xanthene 4a, 4b with sulfonyl chlorides 5a-g and acyl chlorides 7a-d. Structures of the novel amino xanthene compounds and xanthene sulfonamide/carboxamide derivatives were established by their spectral data and elemental analyses. Furthermore, all the synthesized compounds were tested in vitro for their antimicrobial activity. The results were compared with reference standard antibiotics, erythromycin and nystatin. 6c, 6f, 6m and 8b Compounds were found to display most effective antimicrobial activity against a series of bacteria and fungi.
香豆素中间体 4a 和 4b 是通过二甲酮分别与间硝基苯甲醛和对硝基苯甲醛缩合得到的硝基香豆素衍生物 3a 和 3b 的还原得到的。然后，通过氨基香豆素 4a、4b 与磺酰氯 5a-g 和酰氯 7a-d 的反应，合成了香豆素磺酰胺 6a-n 和香豆素甲酰胺衍生物 8a-h。新的氨基香豆素化合物和香豆素磺酰胺/甲酰胺衍生物的结构通过它们的光谱数据和元素分析来确定。此外，所有合成的化合物都在体外进行了抗菌活性测试。结果与参考标准抗生素红霉素和制霉菌素进行了比较。化合物 6c、6f、6m 和 8b 对一系列细菌和真菌表现出最有效的抗菌活性。
