Antimycobacterial natural products: synthesis and preliminary biological evaluation of the oxazole-containing alkaloid texaline
Antimycobacterial natural products: synthesis and preliminary biological evaluation of the oxazole-containing alkaloid texaline
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DOI：
10.1016/j.tetlet.2005.08.119
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发表时间：
2005-10-24
影响因子：
1.8
通讯作者：
Copp, BR
中科院分区：
文献类型：
--
作者：
Giddens, AC;Boshoff, HIM;Copp, BR
为探讨结构与抗结核活性的关系，合成了一种含恶唑的生物碱Tesaline及相关化合物，该生物碱是以前从Amyris texana和Amyfera中分离得到的抗分枝杆菌生物碱。虽然在我们的检测中发现tex-aline没有活性，但更简单的二芳基恶唑更具活性，同时也显示出适度的毒性选择性，导致它们被确定为潜在的先导化合物。(C)2005爱思唯尔有限公司。保留所有权利。
Texaline, an antimycobacterial oxazole-containing alkaloid previously isolated from Amyris texana and A. elemifera, and related compounds have been synthesized in order to explore aspects of the structure-anti tuberculosis activity relationship. While texaline was found to be inactive in our assays, simpler diaryloxazoles were more active whilst also exhibiting modest toxic selectivity, leading to their identification as potential lead compounds. (c) 2005 Elsevier Ltd. All rights reserved.