Synthesis and SAR of novel parenteral anti-pseudomonal cephalosporins: discovery of FR264205

…, T Yamanaka, K Murano, S Okuda, K Kawabata…

Index: Toda, Ayako; Ohki, Hidenori; Yamanaka, Toshio; Murano, Kenji; Okuda, Shinya; Kawabata, Kohji; Hatano, Kazuo; Matsuda, Keiji; Misumi, Keiji; Itoh, Kenji; Satoh, Kenji; Inoue, Satoshi Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 17 p. 4849 - 4852

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Citation Number: 33

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 ...