Synthesis and biological evaluation of novel hygromycin A antibacterial agents.

Michael S Visser,Kevin D Freeman-Cook,Steven J Brickner,Katherine E Brighty,Phuong T Le,Sarah K Wade,Rhonda Monahan, Gary J Martinelli, Kyle T Blair, Dianna E Moore

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

Novel hygromycin A derivatives bearing a variety of functionalized aminocyclitol moieties have been synthesized in an effort to increase the antibacterial activity and drug-like properties of this class of agents. A systematic study of the effect of alkylation and removal of the hydroxyls of the aminocyclitol directed us to a series of alkylated aminocyclitol derivatives with improved gram-positive activity.

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关键词

Hygromycin,Gram-positive,Bacteria,MRSA,Staphylococcus aureus,Aminocyclitol

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