In vitro antimicrobial activities of novel anilinouracils which selectively inhibit DNA polymerase III of gram-positive bacteria
Daly, Jennifer S. ; Giehl, Theodore J. ; Brown, Neal C. ; Zhi, Chengxin ; Wright, George E. ; Ellison, Richard T. III
Citations
Student Authors
Faculty Advisor
Academic Program
Document Type
Publication Date
Subject Area
Files
Embargo Expiration Date
Link to Full Text
Abstract
The 6-anilinouracils are novel dGTP analogs that selectively inhibit the replication-specific DNA polymerase III of gram-positive eubacteria. Two specific derivatives, IMAU (6-[3'-iodo-4'-methylanilino]uracil) and EMAU (6-[3'-ethyl-4'-methylanilino]uracil), were substituted with either a hydroxybutyl (HB) or a methoxybutyl (MB) group at their N3 positions to produce four agents: HB-EMAU, MB-EMAU, HB-IMAU, and MB-IMAU. These four new agents inhibited Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus faecalis, and Enterococcus faecium. Time-kill assays and broth dilution testing confirmed bactericidal activity. These anilinouracil derivatives represent a novel class of antimicrobials with promising activities against gram-positive bacteria that are resistant to currently available agents, validating replication-specific DNA polymerase III as a new target for antimicrobial development.
Source
Antimicrob Agents Chemother. 2000 Aug;44(8):2217-21. doi:10.1128/AAC.44.8.2217-2221.2000. Link to article on publisher's site