Synthesis of Leubethanol derivatives and evaluation against Mycobacterium tuberculosis

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• 作者：Jonathan Perez-Meseguer^a ; Esther del Olmo^b ; ^olmo@usal.es ; Blanca Alanis-Garza^a ; Ricardo Escarcena^b ; Elvira Garza-Gonzá ; lez^a ; Ricardo Salazar-Aranda^a ; Arturo San Feliciano^b ; Noem&iacute ; Waksman de Torres^a ;
• 关键词：Leubethanol ; SAR ; Mycobacterium tuberculosis ; MABA ; Cytotoxicity
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：1 July, 2012
• 卷：20
• 期：13
• 页码：4155-4163
• 文件大小：476 K

摘要

Twenty-five derivatives of the natural diterpene leubethanol, including several potential pro-drugs, with changes in the functionality of the aliphatic chain or modifications of the phenolic group, were synthesized and tested in vitro by the MABA technique for their activity against the H37Rv strain of Mycobacterium tuberculosis. Several compounds showed antimycobacterial potencies similar to that of the lead compound and two of them displayed higher selectivity indexes.