Al-Soud Yaseen A, Al-Dweri Mohammad N, Al-Masoudi Najim A
Department of Chemistry, College of Science, University of Al al-Bayt, Al-Mafraq, Jordan.
Farmaco. 2004 Oct;59(10):775-83. doi: 10.1016/j.farmac.2004.05.006.
A series of 1,5-dialkyl-1,2,4-triazole derivatives of acetic acid alkylidene hydrazides 8-12, the acid 13, 1,5-dialkyl-3-(5-mercapto-4-N-aryl-1H-[1,2,4]-triazol-3-ylmethylene)-1H-[1,2,4] triazoles 14-16, their 1,3,4-oxadiazole analogues 17-21, as well as the 1,2,4-triazolo-indoles 25 and 27 were prepared. The Z/E conformations of some acetic acid alkylidene derivatives were studied by NMR spectroscopy. Most of the target compounds were evaluated in a series of human cancer cell in cultures and none have shown activity except 25 which exhibited remarkable activity against nine cancer types. No in vitro antiviral activity against HIV-1, HIV-2, HSV-1, HSV-2, SV, CV-B4, RSV, P3V, RV, SinV, PTV has been found for all the synthesized compounds.
制备了一系列乙酸亚烃基酰肼的1,5 - 二烷基 - 1,2,4 - 三唑衍生物8 - 12、酸13、1,5 - 二烷基 - 3 - (5 - 巯基 - 4 - N - 芳基 - 1H - [1,2,4] - 三唑 - 3 - 基亚甲基) - 1H - [1,2,4]三唑14 - 16、它们的1,3,4 - 恶二唑类似物17 - 21以及1,2,4 - 三唑并吲哚25和27。通过核磁共振光谱研究了一些乙酸亚烃基衍生物的Z/E构象。在一系列培养的人类癌细胞中对大多数目标化合物进行了评估,除了对九种癌症类型表现出显著活性的25之外,没有化合物显示出活性。对于所有合成化合物,未发现对HIV - 1、HIV - 2、HSV - 1、HSV - 2、SV、CV - B4、RSV、P3V、RV、SinV、PTV的体外抗病毒活性。