Chemistry of pseudomonic acid. Part 16. Aryl and heteroaryl ketone derivatives of monic acid.
The synthesis, antibacterial activities, murine pharmacokinetic and infection model data for a range of aryl and heteroaryl ketone derivatives of monic acid (2a) are reported. The best results were found for the 3-furyl and 2-methoxy thiazol-5-yl analogues.
Abson
A
A
SmithKline Beecham Pharmaceuticals, Brockham Park, Betchworth, Surrey, UK.
Broom
N J
NJ
Coates
P A
PA
Elder
J S
JS
Forrest
A K
AK
Hannan
P C
PC
Hicks
A J
AJ
O'Hanlon
P J
PJ
Masson
N D
ND
Pearson
N D
ND
Pons
J E
JE
Wilson
J M
JM
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D007659:Ketones / Q000737:chemistry; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D008826:Microbial Sensitivity Tests; D016712:Mupirocin / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000494:pharmacology; D018805:Sepsis / Q000188:drug therapy; D013203:Staphylococcal Infections / Q000188:drug therapy; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry
D000900:Anti-Bacterial Agents; D007659:Ketones; D013844:Thiazoles; D016712:Mupirocin