Synthesis of novel 15-membered 8a-azahomoerythromycin A acylides: Consequences of structural modification at the C-3 and C-6 position on antibacterial activity

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• 作者：Dražen Pavlović^a ; ^{drazenpavlovic@rcsi.ie} ; Scott Kimmins^b ; Stjepan Mutak^a
• 关键词：Macrolide antibiotics ; Macrolide resistance ; Acylides ; Structure-activity relationships ; Antibacterial activity ; Heck reaction
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：210-224
• 全文大小：537 K
• 卷排序：125

文摘

New series of acylides were designed and synthesized. Analogs were evaluated against a variety of susceptible and resistant pathogens. Acylide 15na showed an excellent, well balanced antibacterial activity. In vivo efficacy of compound 15na was superior to telithromycin (1). In addition 15na exhibited good oral bioavailability (average F = 42%).