Synthesis of 1,2,3-Triazole Analogues of Lincomycin
Synthesis of 1,2,3-Triazole Analogues of Lincomycin
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DOI：
10.1002/hlca.200890196
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发表时间：
2008-01-01
影响因子：
1.8
通讯作者：
Vasella, Andrea
中科院分区：
文献类型：
--
作者：
Collin, Marie-Pierre;Hobbie, Sven N.;Vasella, Andrea
为了寻找新的抗生素，我们用1，23-三唑环取代了林可霉素I的酰胺部分。1，2，3-三唑10a-10 k通过叠氮化物5与衍生自丙基羟基酸的炔9 k和烷基、芳基或环烷基炔核糖体9a-9 j的“点击反应”以单一区域异构体形式获得。新的类似物被证明对野生型和A2058 G突变体无活性。
In search for ne v antibiotics we replaced the amide moiety of lincomycin I by a 1,23-triazole ring. The 1.2,3-triazoles 10a-10k were obtained as single regioisomers by 'click reaction' of azide 5 with the alkyne 9k, derived from propyl hygric acid, and the alkyl, aryl, or cycloalkyl alkynes ribosomes 9a-9j. The new analogues proved inactive towards wild-type and A2058G mutant.