Synthesis and evaluation of ether and halogenated derivatives of mannopeptimycin glycopeptide antibiotics
作者:Phaik-Eng Sum、David How、Nancy Torres、Peter J. Petersen、Joseph Ashcroft、Edmund I. Graziani、Frank E. Koehn、Tarek S. Mansour
DOI:10.1016/s0960-894x(03)00542-0
日期:2003.8
A number of 6-O-ether and 4-O-ether derivatives of mannopeptimycin-alpha with different steric bulk and lipophilicity were synthesized for structure-activity relationship study. Novel iodo and bromo mannopeptimycin-alpha were also prepared. These compounds were synthesized via electrophilic aromatic substitution. Many of the new ether derivatives exhibited potent antibacterial activity against Gram-positive
合成了许多具有不同空间体积和亲脂性的甘露肽霉素-α的6-O-醚和4-O-醚衍生物用于结构-活性关系研究。还制备了新的碘和溴甘露肽霉素-α。这些化合物是通过亲电芳族取代合成的。许多新的醚衍生物对革兰氏阳性耐药菌株(包括VRE,MRSA和PRSP)表现出有效的抗菌活性。