Mostafa Yaser A-H, Hussein Mostafa A, Radwan Awwad A, Kfafy Abd El-Hamid N
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71526, Egypt.
Arch Pharm Res. 2008 Mar;31(3):279-93. doi: 10.1007/s12272-001-1153-1. Epub 2008 Apr 13.
Certain new derivatives of 1,2,4-triazolo[1,5-a]pyrimidines were synthesized through the reaction of 1,2,4-triazolo[1,5-a]pyrimidine-7-ol with ethyl bromoacetate to afford the ethyl acetate ester, which upon hydrazinolysis gives the corresponding hydrazide. The hydrazide is the key intermediate which was used for the synthesis of the target compounds. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their in vitro antibacterial and antifungal activities. Most of the tested compounds showed comparable results with those of ampicillin and fluconazole reference drugs.
通过1,2,4 - 三唑并[1,5 - a]嘧啶 - 7 - 醇与溴乙酸乙酯反应合成了某些1,2,4 - 三唑并[1,5 - a]嘧啶的新衍生物,得到乙酸乙酯酯,该酯经肼解得到相应的酰肼。酰肼是用于合成目标化合物的关键中间体。通过光谱和元素分析方法确定了新化合物的结构。对合成的化合物进行了体外抗菌和抗真菌活性测试。大多数测试化合物显示出与氨苄青霉素和氟康唑参考药物相当的结果。