Synthesis and biological evaluation of novel hygromycin A antibacterial agents.
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.
Visser
Michael S
MS
Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, United States.
Freeman-Cook
Kevin D
KD
Brickner
Steven J
SJ
Brighty
Katherine E
KE
Le
Phuong T
PT
Wade
Sarah K
SK
Monahan
Rhonda
R
Martinelli
Gary J
GJ
Blair
Kyle T
KT
Moore
Dianna E
DE
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
D000900:Anti-Bacterial Agents; D002934:Cinnamates; D006921:Hygromycin B; C026273:hygromycin A