新型竹桃霉素9-肟。合成、表征及生物活性。
New oleandomycin 9-oximes. Synthesis, characterization and biological activity.
作者信息
Lazarevski G, Kobrehel G, Dokić S, Kolacny-Babić L, Kojić-Prodić B, Janković D, Puntarec V
机构信息
PLIV--Pharmaceutical, Chemical, Food and Cosmetic Industry, Research Institute, Zagreb, Croatia.
出版信息
J Antibiot (Tokyo). 1994 Mar;47(3):349-56. doi: 10.7164/antibiotics.47.349.
A series of the novel oleandomycin 9-oximes has been prepared and characterized by spectroscopic data and X-ray analysis. The antibacterial in vitro activities of the oximes (6-10) were compared with that of oleandomycin (1). Among the novel derivatives the most active compound was 8(R)-methyloleandomycin-9-oxime (9) in contrast ot its 8(S)-isomer (10) which possessed only low potency. Some preliminary pharmacokinetic data of 9 confirmed its activity. Compound 9 has been advanced to further biological study.
已制备了一系列新型竹桃霉素9-肟，并通过光谱数据和X射线分析对其进行了表征。将这些肟（6-10）的体外抗菌活性与竹桃霉素（1）的抗菌活性进行了比较。在这些新型衍生物中，活性最高的化合物是8(R)-甲基竹桃霉素-9-肟（9），而其8(S)-异构体（10）的活性很低。化合物9的一些初步药代动力学数据证实了其活性。化合物9已进入进一步的生物学研究阶段。
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