Chemical modification of erythromycins. IV. Synthesis and biological properties of 6-O-methylerythromycin B.
نویسندگان
چکیده
6-O-Methylerythromycin B has been synthesized from erythromycin B via regioselective methylation of the 6-hydroxyl group in 71% overall yield. This compound shows in vitro antibacterial activity comparable to erythromycins A and B and exhibits superior in vivo activity with improved pharmacokinetic properties.
منابع مشابه
Chemical modification of erythromycins. VI. Structure and antibacterial activity of acid degradation products of 6-O-methylerythromycins A.
Erythromycin A, a useful macrolide antibiotic, is extremely unstable to acid and whenadministered orally undergoes dehydration in vivo to anhydroerythromycin A, an inactive 6,9; 9,12-spiroketal metabolite. 1} In preceding paper,2) we have reported that 6-0-methylerythromycin A (1) was more stable to acid than erythromycin A due to the presence of 6-O-methyl group, which blocks the formation of ...
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ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 43 5 شماره
صفحات -
تاریخ انتشار 1990