甘露糖肽霉素糖肽类抗生素新型苯并恶唑衍生物的合成与活性
Synthesis and activity of novel benzoxazole derivatives of mannopeptimycin glycopeptide antibiotics.
作者信息
Sum Phaik-Eng, How David, Torres Nancy, Newman Howard, Petersen Peter J, Mansour Tarek S
机构信息
Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2003 Aug 4;13(15):2607-10. doi: 10.1016/s0960-894x(03)00512-2.
A series of benzoxazole derivatives of the mannopeptimycin glycopeptide antibiotics was synthesized via a novel benzoxazole formation reaction by treating aminophenol of mannopeptimycin-beta with an aldehyde and DDQ in DMF. Some of these derivatives (e.g., 5b, 5d, 5m, and 7b) showed good activity against Gram-(+) bacteria when compared to the parent compound mannopeptimycin-beta.
通过一种新型苯并恶唑形成反应，用醛和2,3-二氯-5,6-二氰基-1,4-苯醌（DDQ）在N,N-二甲基甲酰胺（DMF）中处理甘露糖肽霉素-β的氨基酚，合成了一系列甘露糖肽霉素糖肽抗生素的苯并恶唑衍生物。与母体化合物甘露糖肽霉素-β相比，其中一些衍生物（如5b、5d、5m和7b）对革兰氏阳性菌表现出良好的活性。
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