丹参酮有关化合物的合成
SYNTHESIS OF SOME COMPOUNDS RELATED TO TANSHINQUINONE
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摘要: 药理试验表明丹参酮IIA及隐丹参酮等有耐缺氧作用。丹参酮IIA等的耐缺氧作用,可能与其邻醌结构有关。我们合成了一些改变醌式结构的丹参酮类似物,经试验,它们的耐缺氧作用减弱。丹参酮IIA由于磺酸基的引入而成水溶性化合物,临床试验对冠心病有效。但存在一些缺点,为了寻找更好的水溶性的丹参酮类化合物,合成了若干丹参酮Ⅰ和IIA的Mannich碱,药理试验表明有较好的抑菌作用。有关心血管方面的药理将另文报道。Abstract: The lipolytic components of Dan Shen (Salvia miltiorrhiza Bunge) were elucidated as a group of diterpene quinones such as tanshinone Ⅰ, tanshinone ⅡA and cryptotanshinone. These compounds were found to increase the resistance of mice to hypoxia in pharmacological tests. Since the activity of these lipolytic components may be due to the presence of the quinone structure, some derivatives with latent quinones have been synthesized. Pharmacological investigations revealed that the biological activity was comparatively weakened.Furthermore, the water soluble sodium sulphonate derivative of tanshinone ⅡA was more active against coronary disease in clinical trial with some side effects. A series of water soluble Mannich bases derived from tanshinones were also prepared. Preliminary pharmacological examination showed that one of them Xa exhibited high bacteriostatic activity against staphylococcus aureus species 18.
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