Fayed Ahmed A, Amr Abd El-Galil E, Al-Omar Mohamed A, Mostafa Elsayed E
Bioorg Khim. 2014 May-Jun;40(3):335-40.
A series of new 3-substituted-7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methylpyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one derivatives were synthesized as antimicrobial agents using 7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methyl-4H-pyrido[3',2':4,5]thieno[3,2-d]-[1,3]oxazin-4-one as a starting compound. Its condensation with substituted aniline derivatives or phenyl hydrazine gave the corresponding N-substituted derivatives. Treatment of the starting compound with hydrazine hydrate afforded the corresponding N-amino derivative, which was reacted with substituted phenylisocyanate and phenylisothiocyanate derivatives to give the corresponding semicarbazides and thiosemicarbazide derivatives. All the newly synthesized compounds were evaluated for their antimicrobial activities in comparison to streptomycin and fusidic acid as positive controls. The structure assignments of the new compounds are based on chemical and spectroscopic evidence.
以7-(2-氯-6-乙氧基吡啶-4-基)-9-(2,4-二氯苯基)-2-甲基-4H-吡啶并[3',2':4,5]噻吩并[3,2-d]-[1,3]恶嗪-4-酮为起始化合物，合成了一系列新型的3-取代-7-(2-氯-6-乙氧基吡啶-4-基)-9-(2,4-二氯苯基)-2-甲基吡啶并[3',2':4,5]噻吩并[3,2-d]嘧啶-4(3H)-酮衍生物作为抗菌剂。它与取代苯胺衍生物或苯肼缩合得到相应的N-取代衍生物。起始化合物与水合肼反应得到相应的N-氨基衍生物，该衍生物与取代的苯基异氰酸酯和苯基异硫氰酸酯衍生物反应得到相应的氨基脲和硫代氨基脲衍生物。与作为阳性对照的链霉素和夫西地酸相比，对所有新合成的化合物进行了抗菌活性评估。新化合物的结构归属基于化学和光谱证据。
