Synthesis and structure-activity relationships of thiotetronic acid analogues of thiolactomycin.
3-Acetyl analogues of thiolactomycin, a thiotetronic acid natural product, were synthesized and profiled against livestock pathogens. Some analogues showed improved activity over thiolactomycin against Staphylococcus aureus and comparable activity against Pasteurella multocida. Several semisynthetically modified analogues of thiolactomycin showed no improvement in activity over thiolactomycin.
Sakya
S M
SM
Veterinary Medicine Pharmaceuticals Discovery, Pfizer Global Research and Development, Pfizer Inc, Groton, CT 06340, USA. sakyas@groton.pfizer.com
Suarez-Contreras
M
M
Dirlam
J P
JP
O'Connell
T N
TN
Hayashi
S F
SF
Santoro
S L
SL
Kamicker
B J
BJ
George
D M
DM
Ziegler
C B
CB
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D013876:Thiophenes; C035068:thiolactomycin