Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594718 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
Fifteen-membered 8a-aza-8a-homoerythromycins derived from either erythromycin or clarithromycin have been acylated to form 4â³-O-propenoyl derivative. These functionalized analogues underwent Michael reaction with primary or secondary amines to afford novel 8a-aza-8a-homoerythromycin-4â³-(3-substituted-amino)propionates. This preparative sequence was adapted so that analogues could be made by parallel synthesis. Among them, 4-quinolone derivatives show particularly good antibacterial potency against macrolide resistant bacteria, comparable or better than azithromycin and telithromycin.
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Authors
Antun Hutinec, Marko Äerek, Gorjana Lazarevski, Vitomir Å unjiÄ, Hana ÄipÄiÄ Paljetak, Sulejman AlihodžiÄ, Vesna ErakoviÄ Haber, Miljenko DumiÄ, NataÅ¡a MarÅ¡iÄ, Stjepan Mutak,