STUDIES OF 7β-[2-(AMINOARYL)ACETAMIDO]- CEPHALOSPORIN DERIVATIVES II. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS IN THE AMINOPYRIMIDINE SERIES

JIRO GOTO; KAZUO SAKANE; YOSHIHARU NAKAI; TSUTOMU TERAJI; TAKASHKI AMIYA

doi:10.7164/antibiotics.37.546

The Journal of Antibiotics

Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820

STUDIES OF 7β-[2-(AMINOARYL)ACETAMIDO]- CEPHALOSPORIN DERIVATIVES

II. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS IN THE AMINOPYRIMIDINE SERIES

JIRO GOTO, KAZUO SAKANE, YOSHIHARU NAKAI, TSUTOMU TERAJI, TAKASHKI AMIYA

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1984 Volume 37 Issue 5 Pages 546-556

DOI https://doi.org/10.7164/antibiotics.37.546

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Abstract

The synthesis and the antibacterial activity of 7β-[2-(aminopyrimidinyl)-2-oxyiminoacetamido] cephalosporins with various substituents at the 3-position in the cephem nucleus are described. The 7β-[2-(4-aminopyrimidin-2-yl)-2-methoxyiminoacetamido]cephalosporin derivative (1) showed significantly higher activity than the corresponding 2-aminopyrimidin-4-yl derivative (2) against Gram-negative bacteria. It was also higher in potency against Escherichia coli and Serratia marcescens than the aminopyridyl compound (4).

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