The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 3-(2-IMIDAZOLYL)THIOMETHYL CEPHALOSPORINS
EIJI NAKANISHIYOSHIAKI OGASAWARAYUKIO SASAKINAOHIKO YASUDA
Author information
JOURNAL FREE ACCESS

1989 Volume 42 Issue 1 Pages 54-62

Details
Abstract

The synthesis and structure-activity relationships of a series of 3-(2-imidazolyl)thiomethyl cephalosporins are described. Among the compounds, 7β-[2-(2-amino-1, 3-thiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3-[(4, 5-dicarboxyimidazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid (1) exhibited potent activity against both Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa. We also estimated lipophilicity of the compounds from the chromatographic log k' value of reversed-phase HPLC. The relationship between lipophilicity and biological activity showed that compound 1 had the most suitable lipophilicity.

Content from these authors
© Japan Antibiotics Research Association
Previous article Next article
feedback
Top