RING-REDUCED MACROLIDE ANTIBIOTIC

Novel 12-membered lactone and 11-membered lactone derivatives of erythromycin, having antimicrobial activity against certain Gram-positive pathogens such as Streptococcus pyogenes and Gram-negative cocci such as Haemophilus influenzae, and useful as intermediates to other macrolide derivatives, are...

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Hauptverfasser: HAABAATO ANDORIYUU KAASUTO, JIYURII AN UINDO
Format: Patent
Sprache:eng
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Zusammenfassung:Novel 12-membered lactone and 11-membered lactone derivatives of erythromycin, having antimicrobial activity against certain Gram-positive pathogens such as Streptococcus pyogenes and Gram-negative cocci such as Haemophilus influenzae, and useful as intermediates to other macrolide derivatives, are disclosed. They have the formula (A) R is hydrogen or C1-C5-alkanoyl; R is -N(CH3)2 or -N(CH3)2->O; and either a) R and R taken together form a bond, and R and R are 1) either both hydroxyl or 2) taken together form a bond; or b) each of R and R taken together and R and R taken together form a keto group; provided that, when R is an (a) group and R is -N(CH3)2, both R and R together and R and R together cannot form a bond; or a salt thereof. b