Synthesis of novel 5,6,7,8,9,10-hexahydropyrimido[4,5-b]quinoline derivatives for antimicrobial and anti-oxidant evaluation
作者:Rasha S. Gouhar、Wael S. I. Abou-Elmagd、Magdy I. El-Zahar、Mohsen M. Kamel、Dina H. El-Ghonamy
DOI:10.1007/s11164-016-2699-0
日期:2017.3
alcohols to give the carboxylic esters 5 and with hydrazine to give the carbohydrazide 8. Compound 8 reacted with aldoses to give the corresponding polyhydroxy(-)alkyl Schiff bases 9, which upon reaction with thioglycolic acid afforded the thiazolidinone-C-acyclic nucleosides 10. Several other pyrimidoquinolines incorporated to oxadiazole, iminothiazolidinones and thiadiazoles were synthesized starting from
由于嘧啶基喹啉具有众所周知的化学治疗活性,因此合成了一系列新的标题化合物,并对其生物学性进行了抗微生物和抗氧化活性筛选。制备中间体化合物2-氨基-1-环己基-4-(3,4-二甲氧基苯基)-1,4,5,6,7,8-六氢喹啉-3-腈(2),使其与草酰氯制得相应的战略原料,10-环己基-5-(3,4-二甲氧基苯基)-4-氧代-3,4,5,6,7,8,9,10-八氢嘧啶基[4,5- b]喹啉-2-羰基氯3。化合物3与胺进行各种反应,得到相应的羧酸酰胺4,与醇进行化学反应,得到羧酸酯5。并与肼一起生成碳酰肼8。化合物8与醛糖反应得到相应的多羟基(-)烷基席夫碱9,其与巯基乙酸反应后得到噻唑烷酮-C-无环核苷10。从2-carbohydrazide衍生物8开始合成了结合到恶二唑,亚胺基噻唑烷酮和噻二唑的其他几种嘧啶喹啉。大多数新制备的衍生物显示出对革兰氏+ ve和革兰氏ve细菌相当大的抗菌活性和抗氧化活性。