0

Design and Synthesis via Click Chemistry of 8,9-anhydroerythromycin A 6,9-hemiketal Analogues With anti-MRSA and -VRE Activity

Akihiro Sugawara, Toshiaki Sunazuka, Tomoyasu Hirose, Kenichiro Nagai, Yukie Yamaguchi, Hideaki Hanaki, K Barry Sharpless, Satoshi Omura

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6340-4.

PMID: 17869508

Abstract:

An erythromycin analogue, 11,12-di-O-iso-butyryl-8,9-anhydroerythromycin A 6,9-hemiketal (1b), was found to be a potential anti-MRSA and anti-VRE agent. The use of copper catalyzed azide-acetylene cycloaddition, and click chemistry, readily provided 10 types of triazole analogues of 1b in good to nearly quantitative yield. Among the library, 5b exhibited activity against MRSA and VRE bacterial strains, representing more than twice the potency of 1b.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP23893132 Anhydroerythromycin A Anhydroerythromycin A 23893-13-2 Price
qrcode