Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases.
A series of novel aminoacyl adenylate mimics has been prepared and evaluated for their inhibitory activity against aminoacyl-tRNA synthetases. Several of these thiazole derivatives displayed potent and selective enzyme activity against both Gram-positive and Gram-negative bacteria.
Yu
X Y
XY
Department of Medicinal Chemistry, Cubist Pharmaceuticals, Inc., Cambridge, MA 02139, USA.
Hill
J M
JM
Yu
G
G
Wang
W
W
Kluge
A F
AF
Wendler
P
P
Gallant
P
P
D000604:Amino Acyl-tRNA Synthetases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004926:Escherichia coli / Q000201:enzymology; D006801:Humans; D013211:Staphylococcus aureus / Q000201:enzymology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D013844:Thiazoles; D000604:Amino Acyl-tRNA Synthetases