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Comparative Study
, 18 (17), 4849-52

Synthesis and SAR of Novel Parenteral Anti-Pseudomonal Cephalosporins: Discovery of FR264205

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Comparative Study

Synthesis and SAR of Novel Parenteral Anti-Pseudomonal Cephalosporins: Discovery of FR264205

Ayako Toda et al. Bioorg Med Chem Lett.

Abstract

We describe herein the synthesis and biological evaluation of a series of novel cephalosporins with potent activity against Pseudomonas aeruginosa. Introduction of various amino groups to the 4-position of a 3-amino-2-methylpyrazole cephalosporin 3-side chain resulted in enhanced MIC values against multiple Pseudomonas aeruginosa strains and ultimately led to the discovery of FR264205 (15) with excellent anti-bacterial activity and weak convulsion effect by direct intracerebroventricular injection assay.

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