title: Synthesis and biological evaluation of novel hygromycin A antibacterial agents.
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.
authors.affiliation: Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, United States.
authors.forename: Michael S
authors.initials: MS
authors.lastname: Visser
authors.forename: Kevin D
authors.initials: KD
authors.lastname: Freeman-Cook
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Brickner
authors.forename: Katherine E
authors.initials: KE
authors.lastname: Brighty
authors.forename: Phuong T
authors.initials: PT
authors.lastname: Le
authors.forename: Sarah K
authors.initials: SK
authors.lastname: Wade
authors.forename: Rhonda
authors.initials: R
authors.lastname: Monahan
authors.forename: Gary J
authors.initials: GJ
authors.lastname: Martinelli
authors.forename: Kyle T
authors.initials: KT
authors.lastname: Blair
authors.forename: Dianna E
authors.initials: DE
authors.lastname: Moore
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002934:Cinnamates / Q000138:chemical synthesis* / Q000494:pharmacology*; D006921:Hygromycin B / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D008826:Microbial Sensitivity Tests
chemical_list: D000900:Anti-Bacterial Agents; D002934:Cinnamates; D006921:Hygromycin B; C026273:hygromycin A