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香豆素衍生物的合成及作为分枝杆菌(BCG)抑制剂的生物评价。

Synthesis and biological evaluation of coumarin derivatives as inhibitors of Mycobacterium bovis (BCG).

机构信息

Department of Life Science Engineering, Faculty of New Science and Technology, University of Tehran, Tehran, Iran.

出版信息

Chem Biol Drug Des. 2012 Dec;80(6):929-36. doi: 10.1111/cbdd.12044.

Abstract

The coumarin compounds are an important class of biologically active molecules, which have attractive caught the attention of many organic and medicinal chemists, due to potential pharmaceutical implications and industrial applications. We herein report the one-pot procedure for the efficient synthesis of coumarin derivatives using commercially available substrates via isocyanide-based multicomponent condensation reactions. These compounds were evaluated for anti-mycobacterium activity against Mycobacterium bovis (Bacillus Calmette-Guerin). The preliminary results indicated that all of the tested compounds showed relatively good activity against the test organism. The compounds 7e, 7l, and 7m showed high anti-tuberculosis activity.

摘要

香豆素类化合物是一类重要的具有生物活性的分子,由于具有潜在的药物意义和工业应用,引起了许多有机和药物化学家的关注。在这里,我们报告了一种使用市售底物通过异氰化物基多组分缩合反应高效合成香豆素衍生物的一锅法。这些化合物被评估了对分枝杆菌(卡介苗)的抗结核活性。初步结果表明,所有测试的化合物对测试生物都表现出相对较好的活性。化合物 7e、7l 和 7m 表现出高的抗结核活性。

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