Ureas of 5-aminopyrazole and 2-aminothiazole inhibit growth of gram-positive bacteria.
Ureas of 5-aminopyrazole and 2-aminothiazole emerged as lead compounds from a high-throughput screen assaying the growth of Staphylococcus aureus. Structure-activity relationships were developed for each compound series. Several compounds were also tested for activity against drug resistant strains of S. aureus in vivo.
Kane
John L
JL
Genzyme Drug Discovery and Development, Genzyme Corp, Cambridge MA 02139, USA. john.crane@genzyme.com
Hirth
Bradford H
BH
Liang
Beirong
B
Gourlie
Brian B
BB
Nahill
Sharon
S
Barsomian
Gary
G
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D011720:Pyrazoles; D013844:Thiazoles; D014508:Urea