4-Thiazolidinone and 1-thia-3,4,9-triaza fluorene conjugates: synthesis, characterization and antimicrobial screening
作者:Om Prakash Agrawal、Pankaj Kumar Sonar、Shailendra K. Saraf
DOI:10.1007/s00044-012-0200-1
日期:2013.4
derivatives have been synthesized by the condensation of isatin/5-chloroisatin with thiosemicarbazide to yield thiosemicarbazones, which were then cyclized to form corresponding thia-3,4,9-triaza-fluoren-2-ylamines. These were reacted with substituted aldehydes to give corresponding Schiff bases, which were cyclized using thioglycolic acid in the presence of zinc chloride to obtain the 4-thiazolidinone
一些新的4-噻唑烷酮衍生物是通过将isatin / 5-氯异丁嗪与硫代氨基脲缩合而合成的,得到硫代氨基脲,然后将其环化形成相应的thia-3,4,9-三氮杂-芴-2-基胺。使它们与取代的醛反应以得到相应的席夫碱,将其在氯化锌存在下使用巯基乙酸环化以获得4-噻唑烷酮衍生物。所有合成的化合物都通过光谱(IR,MS和NMR)和元素分析进行了表征。将化合物筛选它们对革兰氏阳性菌的抗菌活性(枯草芽孢杆菌,金黄色葡萄球菌,短小芽孢杆菌和中号。藤黄微球菌),革兰氏阴性细菌(铜绿假单胞菌,大肠杆菌和荧光假单胞菌)以及通过琼脂扩散法对黑曲霉和产黄青霉的抗真菌活性。这些化合物的最小抑菌浓度也通过试管稀释法确定。发现所有化合物的抗微生物效力是浓度依赖性的。两种化合物-2-甲基-3-(1-硫杂-3,4,9-三氮杂芴-2-基)-噻唑烷丁-4-酮(7aI)和2-萘-1-基-3-(1 -thia-3,4,9-三氮杂