Galabov A S, Velichkova E, Karparov A, Sidzhakova D, Danchev D, Chakova N
Arzneimittelforschung. 1984;34(1):9-14. doi: 10.1002/chin.198419231.
24 derivatives of tetrahydro-2(1H)-pyrimidinone and related compounds were tested in vitro for antiviral activity against representatives of six viral taxonomic groups. The screening was carried out by a two-stage procedure including the agar-diffusion plaque-inhibition test and the one-step growth cycle setup. A distinct activity of three mono- and bis-morpholinomethyl derivatives of tetrahydro-2(1H)-pyrimidinone (THP), 1,3-bis(piperidinomethyl)-THP, the 1-morpholinomethyl derivative of tetrahydro-2(1H)-pyrimidinethione (THPT) and the related N,N'-bis(morpholinomethyl)-urea against the fowl plague virus was established. In the one-step growth cycle setup these compounds inhibited 87.5-99.6% of the infectious virus yield. Two of the compounds, namely 1-morpholinomethyl derivatives of THP and THPT manifested a strong inhibitory effect on the reproduction of Semliki Forest virus as well, exceeding 99.9% in the one-step growth cycle test. A borderline effect was observed in some derivatives against vaccinia virus and Newcastle disease virus. The structure-activity relationship of this group of compounds is discussed.
对24种四氢-2(1H)-嘧啶酮衍生物及相关化合物进行了体外测试，以检测其对六个病毒分类群代表的抗病毒活性。筛选采用两阶段程序进行，包括琼脂扩散空斑抑制试验和一步生长周期实验。确定了三种四氢-2(1H)-嘧啶酮（THP）的单和双吗啉甲基衍生物、1,3-双（哌啶甲基）-THP、四氢-2(1H)-嘧啶硫酮（THPT）的1-吗啉甲基衍生物以及相关的N,N'-双（吗啉甲基）脲对禽瘟病毒具有明显活性。在一步生长周期实验中，这些化合物抑制了87.5 - 99.6%的感染性病毒产量。其中两种化合物，即THP和THPT的1-吗啉甲基衍生物对Semliki森林病毒的复制也表现出强烈的抑制作用，在一步生长周期试验中超过99.9%。在一些衍生物中观察到对痘苗病毒和新城疫病毒的临界效应。讨论了这组化合物的构效关系。
