engleski

Novel 8a-aza-8a-homoerythromycin—400-(3- substituted-amino)propionates with broad spectrum antibacterial activity

Fifteen-membered 8a-aza-8a-homoerythromycins derived from either erythromycin or clarithromycin have been acylated to form 400-O-propenoyl derivative. These functionalized analogues underwent Michael reaction with primary or secondary amines to afford novel 8a-aza-8a- homoerythromycin—400- (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.

macrolide; azalide; 8a-aza-8a-Homoerythromycin—400-(3-substituted-amino)propionates; antibacterial activity; rResistance

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