SALTS OF 5,5'-ARYLIDENEBISBARBITURIC AND 5,5'-ARYLIDENEBIS(2-THIOBARBITURIC) ACIDS AND 5,5'-ARYLIDENEBIS(2-THIOBARBITURIC) ACIDS HAVING AN ANTIBACTERIAL, ANTI-CHLAMYDIAL, ANTIVIRAL AND IMMUNO-MODULATING ACTIVITY
申请人:Tets, Viktor Veniaminovich
公开号:EP1043318A1
公开(公告)日:2000-10-11
The present invention relates to the production of new chemical substances having an anti-microbial, antiviral, immuno-modulating and anti-tumoral activity. This invention more precisely relates to the synthesis of new substances consisting of 5,5'-arylidenebis(2-thiobarbituric) acids and in salts of 5,5'-arylidenebisbarbituric and 5,5'-arylidenebis(2-thiobarbituric) acids of general formula (I) where X is oxygen or sulphur. R1 is hydrogen, a nitro group or an alkoxy group, R2 is hydrogen, a nitro group, an alkoxy group or halogen and Cat+ is a proton or a pyridin- or 2-hydroxyethylammonium-cation. In the preferred embodiments of these substances, the following conditions are observed:
This invention also relates to eight synthesis instances of these substances, to three tables representing the chemical and physical characteristics of the substances thus obtained and to the results of five series of experiments. These synthesis instances, tables and results demonstrate the biological properties of these substances on myco-bacteria, on herpes viruses and on Chlamydia trachomatis as well as their interferon-inducing activity and the absence of acute toxicity.
本发明涉及生产具有抗微生物、抗病毒、免疫调节和抗肿瘤活性的新化学物质。更确切地说,本发明涉及由 5,5'-亚芳基双(2-硫代巴比妥酸)和通式(I)的 5,5'-亚芳基双巴比妥酸和 5,5'-亚芳基双(2-硫代巴比妥酸)的盐组成的新物质的合成 其中 X 是氧或硫。R1 是氢、硝基或烷氧基,R2 是氢、硝基、烷氧基或卤素,Cat+ 是质子或吡啶或 2-羟乙基铵阳离子。在这些物质的优选实施方案中,应遵守以下条件:
本发明还涉及这些物质的八个合成实例、代表由此获得的物质的化学和物理特性的三个表格以及五个系列实验的结果。这些合成实例、表格和结果表明了这些物质对霉菌、疱疹病毒和沙眼衣原体的生物特性,以及它们的干扰素诱导活性和无急性毒性。