新型半合成糖肽类抗生素，对耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素肠球菌（VRE）具有活性：氯东方霉素B的双修饰水溶性衍生物。
Novel semi-synthetic glycopeptide antibiotics active against methicillin-resistant staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE): doubly-modified water-soluble derivatives of chloroorienticin B.
作者信息
Yoshida Osamu, Yasukata Tatsuro, Sumino Yukihito, Munekage Tadashi, Narukawa Yukitoshi, Nishitani Yasuhiro
机构信息
Discovery Research Laboratories, Shionogi & Co., Ltd., Sagisu 5-12-4, Fukushima-ku, 553-0002, Osaka, Japan.
出版信息
Bioorg Med Chem Lett. 2002 Nov 4;12(21):3027-31. doi: 10.1016/s0960-894x(02)00664-9.
Abstract
A series of N-alkylated and aminomethylated derivatives of chloroorienticin B, a vancomycin-related glycopeptide antibiotic, were synthesized. Doubly-modified derivatives having both hydrophobic and hydrophilic substituents exhibited potent antibacterial activity against MRSA and VRE along with considerable water-solubility.
摘要
合成了一系列与万古霉素相关的糖肽抗生素氯定向霉素B的N-烷基化和氨甲基化衍生物。具有疏水和亲水取代基的双修饰衍生物对耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素肠球菌（VRE）表现出强效抗菌活性，同时具有相当的水溶性。
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