硫代色满-4-酮衍生物的合成与评价及其作为潜在利什曼原虫药物的研究。
Synthesis and Evaluation of Thiochroman-4-One Derivatives as Potential Leishmanicidal Agents.
机构信息
Química Orgánica de Productos Naturales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, calle 70 No. 52-21, Medellin A.A 1226, Colombia.
PECET-Facultad de Medicina, Universidad de Antioquia, calle 70 No. 52-21, Medellin A.A 1226, Colombia.
出版信息
Molecules. 2017 Nov 29;22(12):2041. doi: 10.3390/molecules22122041.
The S-containing heterocyclic compounds benzothiopyrans or thiochromones stand out as having promising biological activities due to their structural relationship with chromones (benzopyrans), which are widely known as privileged scaffolds in medicinal chemistry. In this work, we report the synthesis of 35 thiochromone derivatives and the in vitro antileishmanial and cytotoxic activities. Compounds were tested against intracellular amastigotes of and cytotoxic activity against human monocytes (U-937 ATCC CRL-1593.2). Compounds bearing a vinyl sulfone moiety, , , , , and , displayed the highest antileishmanial activity, with EC values lower than 10 μM and an index of selectivity over 100 for compounds and . When the double bond or the sulfone moiety was removed, the activity decreased. Our results show that thiochromones bearing a vinyl sulfone moiety are endowed with high antileishmanial activity and low cytotoxicity.
含硫杂环化合物苯并噻喃或硫代色满酮因其与色满（苯并吡喃）的结构关系而引人注目，色满被广泛认为是药物化学中的优势骨架。在这项工作中，我们报告了 35 种硫代色满酮衍生物的合成及其体外抗利什曼原虫和细胞毒性活性。对化合物进行了针对 和细胞内无鞭毛体的测试，并对人单核细胞（U-937 ATCC CRL-1593.2）进行了细胞毒性活性测试。含有乙烯砜部分的化合物 、 、 、 、 和 表现出最高的抗利什曼原虫活性，EC 值低于 10 μM，化合物 和 的选择性指数超过 100。当双键或砜部分被去除时，活性降低。我们的结果表明，含有乙烯砜部分的硫代色满酮具有高抗利什曼原虫活性和低细胞毒性。
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