Design, synthesis, antimicrobial activity and molecular docking studies of some novel di-substituted sulfonylquinoxaline derivatives
作者:Yousry A. Ammar、Awatef A. Farag、Abeer M. Ali、Ahmed Ragab、Ahmed A. Askar、Doaa M. Elsisi、Amany Belal
DOI:10.1016/j.bioorg.2020.104164
日期:2020.11
quinoxaline derivatives 11a-c. Additionally triazolo and pyrazolyl quinoxaline derivatives 12–14 were obtained through the reaction of compound 11a with phenyl isothiocyanate, formylpyrazole and ethyl acetoacetate. All the synthesized compounds were screened for their antibacterial and antifungal activities. Compounds 7a, 9b, 10a, 10c, 10f and 11c showed good to moderate antimicrobial activity against
通过邻苯二胺与草酸反应,然后用过量的氯磺酸进行氯磺化反应,制得2,3-二氧-1,2,3,4-四氢喹喔啉-6-磺酰氯1。一系列新sulfonylquinoxaline衍生物的2 - 6在化合物反应,得到1与不同类型的胺。2,3-二氯-6- morpholinosulfonylquinoxaline衍生物6进行进一步的化学反应,得到6-吗啉代的许多衍生物2,3- disubstitutedquinoxalines,从而化合物的反应6具有不同的仲胺,得到单和二仲氨基喹喔啉衍生物7 - 10取决于两个氯原子的反应性差异。化合物7提供的肼基喹喔啉衍生物11a-c的水合肼解。此外三唑和吡唑基喹喔啉衍生物12 - 14是通过化合物的反应获得11A与异硫氰酸苯酯,甲酰基和乙酰乙酸乙酯。筛选所有合成的化合物的抗菌和抗真菌活性。化合物7a,9b,10a,10c,10f和11c对被测革兰氏阳性,革兰氏阴性细菌和