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

doi:10.1016/j.bmcl.2010.08.139

Synthesis and biological evaluation of novel hygromycin A antibacterial agents

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6730-4. doi: 10.1016/j.bmcl.2010.08.139. Epub 2010 Sep 21.

Authors

Michael S Visser¹, 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

Affiliation

¹ Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, United States.

PMID: 20864341
DOI: 10.1016/j.bmcl.2010.08.139

Abstract

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.

MeSH terms

Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / pharmacology*
Cinnamates / chemical synthesis*
Cinnamates / pharmacology*
Hygromycin B / analogs & derivatives*
Hygromycin B / chemical synthesis
Hygromycin B / pharmacology
Microbial Sensitivity Tests

Substances

Anti-Bacterial Agents
Cinnamates
Hygromycin B
hygromycin A