CEPHALOSPORIN ANTIBIOTICS: I. SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIPS OF 3-THIAZOLIOMETHYL DERIVATIVES

The synthesis and the structure-activity relationships of 3-thiazoliomethyl cephalosporins are described. In a series of these parenteral compounds, 2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido group was found to be a favorable substituent for the C-7 position of the cephem nucleus. They show...

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Bibliographic Details
Published in:Journal of antibiotics 1991/08/25, Vol.44(8), pp.854-863
Main Authors: NAKAYAMA, EIJI, FUJIMOTO, KOICHI, MURAMATSU, SHIGEKI, MIYAUCHI, MASAO, WATANABE, KATSUHIKO, IDE, JUNYA
Format: Article
Language:English
Subjects:
Cephalosporins - chemical synthesis
Cephalosporins - chemistry
Cephalosporins - pharmacology
Microbial Sensitivity Tests
Structure-Activity Relationship
Thiazoles - chemical synthesis
Thiazoles - chemistry
Thiazoles - pharmacology
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Summary:The synthesis and the structure-activity relationships of 3-thiazoliomethyl cephalosporins are described. In a series of these parenteral compounds, 2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido group was found to be a favorable substituent for the C-7 position of the cephem nucleus. They showed potent antibacterial activity against both Gram-positive and Gram-negative bacteria including some β-lactamase producing species.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.44.854