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二丁基氧化锡法在泰乐菌素C-4''位区域选择性酰化和烷基化中的应用

Application of dibutyltin oxide method to regioselective acylation and alkylation of tylosin at C-4''.

作者信息

Kiyoshima K, Sakamoto M, Ishikura T, Fukagawa Y, Yoshioka T, Naganawa H, Sawa T, Takeuchi T

出版信息

Chem Pharm Bull (Tokyo). 1989 Apr;37(4):861-5. doi: 10.1248/cpb.37.861.

DOI:10.1248/cpb.37.861
PMID:2766418
Abstract

4''-O-Acyl-, 4''-O-alkyl- and 4''-deoxy-tylosin derivatives were synthesized using 2'-O-acetyl-3'',4''-O-(dibutyl-stannio)tylosin as a synthetic intermediate. The in vitro biological evaluation showed that the new derivatives were active against macrolide-resistant clinical isolates of bacteria and mycoplasmas, and that they were resistant to hepatic esterase.

摘要

以2'-O-乙酰基-3'',4''-O-(二丁基锡)泰乐菌素为合成中间体,合成了4''-O-酰基-、4''-O-烷基-和4''-脱氧-泰乐菌素衍生物。体外生物学评价表明,这些新衍生物对耐大环内酯类临床分离细菌和支原体具有活性,并且对肝脏酯酶具有抗性。

相似文献

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Application of dibutyltin oxide method to regioselective acylation and alkylation of tylosin at C-4''.二丁基氧化锡法在泰乐菌素C-4''位区域选择性酰化和烷基化中的应用
Chem Pharm Bull (Tokyo). 1989 Apr;37(4):861-5. doi: 10.1248/cpb.37.861.
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Biological properties of new acyl derivatives of tylosin.
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Binding of 3-O-acetyl-4"-O-isovaleryltylosin to ribosomes from a macrolide-resistant strain of Staphylococcus aureus.3-O-乙酰基-4″-O-异戊酰泰乐菌素与耐大环内酯类金黄色葡萄球菌菌株核糖体的结合
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In vitro activity of YM133, a new semisynthesized macrolide.新型半合成大环内酯类药物YM133的体外活性
Antimicrob Agents Chemother. 1991 Jul;35(7):1370-5. doi: 10.1128/AAC.35.7.1370.