A new type of ketolides bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether synthesis and structure–activity relationships

…, T Yasukata, K Nishi, Y Narukawa, K Uotani…

Index: Nomura, Takashi; Iwaki, Tsutomu; Yasukata, Tatsuro; Nishi, Koichi; Narukawa, Yukitoshi; Uotani, Koichi; Hori, Toshihiko; Miwa, Hideaki Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 24 p. 6615 - 6628

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Citation Number: 18

Abstract

A new type of ketolides, bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether and a cyclic carbonate at the C-11, 12 position was prepared and the antibacterial activities of the compounds were evaluated. Some of the derivatives showed potent antibacterial activity against both Haemophilus influenzae and Streptococcus pneumoniae, which are clinically important respiratory tract pathogens. Among the derivatives prepared, compound 5s with ...