病原体灭活核酸嵌入剂的合成

Synthesis of pathogen inactivating nucleic acid intercalators.

作者信息

Csuk René, Barthel Alexander, Brezesinski Thorsten, Raschke Christian

机构信息

Institut für Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Strasse 2, 06120 Halle (Saale), Germany.

出版信息

Eur J Med Chem. 2004 Nov;39(11):975-88. doi: 10.1016/j.ejmech.2004.07.011.

DOI:10.1016/j.ejmech.2004.07.011

PMID:15501547

Abstract

A series of antiviral compounds consisting of an intercalating acridine derived part, a spacer region and a reactive EDTA-derived conjugate was synthesized in an easy sequence starting from 1,omega-alkyldiamines. As shown in model screenings, in the presence of ascorbic acid the Fe-complexes of these compounds reduced the phage-titer of MS2-phages by several logarithmic decades.

摘要

一系列由嵌入吖啶衍生部分、间隔区和反应性乙二胺四乙酸衍生共轭物组成的抗病毒化合物，以1,ω-烷基二胺为起始原料，通过简单的步骤合成。如模型筛选所示，在抗坏血酸存在下，这些化合物的铁络合物使MS2噬菌体的噬菌体效价降低了几个对数级。