无血小板聚集活性的N-糖基硫脲基无苷元瑞斯托菌素
N-glycosylthioureido aglyco-ristocetins without platelet aggregation activity.
作者信息
Sztaricskai Ferenc, Pintér Gábor, Röth Erzsébet, Herczegh Pál, Kardos Szilvia, Rozgonyi Ferenc, Boda Zoltán
机构信息
Department of Pharmaceutial Chemistry, University of Debrecen.
出版信息
J Antibiot (Tokyo). 2007 Aug;60(8):529-33. doi: 10.1038/ja.2007.68.
The water-soluble N-methoxy-PEG-yl-, N-beta-D-glucopyranosyl- and N-beta-D-maltosylthioureido aglyco-ristocetin were prepared which, in contrast to ristocetin A, did not induce thrombocyte aggregation. The antibacterial activity of N-beta-D-maltosylthioureido aglyco-ristocetin A against MRSA was comparable to that of ristocetin A, while its activity against Enterococcus faecalis (VRE, TSE) is somewhat stronger when compared to those of vancomycin and ristocetin A.
制备了水溶性的N-甲氧基-聚乙二醇基-、N-β-D-吡喃葡萄糖基-和N-β-D-麦芽糖基硫脲基去糖基瑞斯托菌素，与瑞斯托菌素A不同，它们不会诱导血小板聚集。N-β-D-麦芽糖基硫脲基去糖基瑞斯托菌素A对耐甲氧西林金黄色葡萄球菌（MRSA）的抗菌活性与瑞斯托菌素A相当，而与万古霉素和瑞斯托菌素A相比，其对粪肠球菌（VRE、TSE）的活性略强。
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