STUDIES ON BETA-LACTAM ANTIBIOTICS .3. SYNTHESES AND ANTIBACTERIAL ACTIVITIES OF NEW 3-(1,3-DITHIOLAN-2-YL)CEPHALOSPORINS, YM-22508, YM-16457 AND THEIR PRODRUG-TYPE ESTERS

被引：7

作者：

NAGANO, N

SATOH, M

HARA, R

机构：

[1] Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd., Ibaraki 305, 21 Miyukigaoka, Tsukuba City

来源：

JOURNAL OF ANTIBIOTICS | 1991年 / 44卷 / 04期

关键词：

D O I：

10.7164/antibiotics.44.422

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

The syntheses and biological activities of new 7-beta-[(Z)-2-(2-amino-4-thiazolyl)-2-hydroxy-iminoacetamido]-3-(1,3-dithiolan-2-yl)-3-cephem-4-carboxylic acid (YM-22508, 1a), 7-beta-[(Z)-2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-(1,3-dithiolan-2-yl)-3-cephem-4-carboxylic acid (YM-16457, 1d) and their prodrug-type esters are described. Among them, YM-22561 (1c), the 1-acetoxyethyl ester of 1a, showed good in vivo efficacy in mice against infections of Staphylococcus aureus Smith, Streptococcus pyogenes S 23 and Escherichia coli NY-17 and a long plasma T1/2 in mice.

引用

页码：422 / 428

页数：7

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