3位酮基红霉衍生物的半合成及其抗菌活性研究

设计合成了３位酮基－９－（２－甲氧基异丙基）－肟红霉素及其中间体，抗菌活性检测表明，目标化合物及其中间体均有不同程度的抗菌活性，其中Ｋ３和Ｋｍ对革兰氏阳性菌抗菌活性与红霉素相似，而Ｋｍ对红霉素耐药菌有较强作用。

Studies on the semi-synthesis and antibacterial activity of 3-ketoerythromycin derivatives

Recently, Roussel Ulcaf has removed the cladinose sugar of clarithromycin through acid catalyzed hydrolysis and the resulting hydroxyl group was oxidized to a ketone functionality at C 3 position. This compound, called ketolide, was further modified to produce derivatives that showed erythromycin like activity against several susceptible organisms and improved activity against several resistant organisms including inducible and constitutive types. We also devised some ketolides expecting to find compound possessing stronger activity. Our synthetic strategy was from erythromycin A to the desired ketolides using oximation, hydrolysis, protection, oxidation, deprotection and condensation. These prepared compounds were tested in vitro against both erythromycin susceptible and erythromycin resistant organisms using standard agar dilution method.