Novel ketolide antibiotics with a fused five-membered lactone ring––synthesis, physicochemical and antimicrobial properties

…, W Arnold, A Stämpfli, A Schmitt-Hoffmann…

Index: Hunziker, Daniel; Wyss, Pierre-C.; Angehrn, Peter; Mueller, Aranka; Marty, Hans-Peter; Halm, Remy; Kellenberger, Laurenz; Bitsch, Veronique; Biringer, Gerard; Arnold, Wolf; Staempfli, Andreas; Schmitt-Hoffmann, Anne; Cousot, Denis Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 13 p. 3503 - 3519

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Citation Number: 28

Abstract

In an effort to find novel semisynthetic macrolides with extended antibacterial spectrum and improved activity we prepared a series of compounds based on commercially available clarithromycin, a potent and safe antimicrobial agent of outstanding clinical and commercial interest. According to the literature, improvement of antibacterial activity of erythromycin type antibiotics can be achieved by introduction of fused heterocycles such as cyclic ...