Lyakhov S A, Suveyzdis Y I, Litvinova L A, Andronati S A, Rybalko S L, Dyadyun S T
A. V. Bogatsky Physico-Chemical Institute, National Academy of Sciences of Ukraine, Odessa, Ukraine.
Pharmazie. 2000 Oct;55(10):733-6.
Nine bis-acridine derivatives have been synthesized in search of structures with antiviral properties. Synthesis of target compounds was provided by a standard peptide-like coupling procedure using aliphatic diamines and protected amino acids following protective group removing and acridinylation by means of 9-methoxyacridine. Two out of nine compounds tested demonstrate high protective activity of Vero cells against HSV infection. Antiviral activity was observed only for compounds containing a pentamethylene fragment as a linker. The alanyl-containing derivative was less active than those containing valyl- and phenylalanyl. Most of synthesized compounds were less toxic than N,N'-bis-(acridinyl) hexamethylenediamine.
为了寻找具有抗病毒特性的结构，已合成了九种双吖啶衍生物。目标化合物的合成是通过标准的类肽偶联程序进行的，该程序使用脂肪族二胺和受保护的氨基酸，经过保护基团去除后，再通过9-甲氧基吖啶进行吖啶化反应。在测试的九种化合物中，有两种对Vero细胞抵抗单纯疱疹病毒（HSV）感染表现出高保护活性。仅含有亚戊基片段作为连接基的化合物观察到了抗病毒活性。含丙氨酰基的衍生物比含缬氨酰基和苯丙氨酰基的衍生物活性低。大多数合成化合物的毒性低于N,N'-双（吖啶基）六亚甲基二胺。
