title: Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases.
abstract: 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.
authors: Department of Medicinal Chemistry, Cubist Pharmaceuticals, Inc., Cambridge, MA 02139, USA.
authors: X Y
authors: XY
authors: Yu
authors: J M
authors: JM
authors: Hill
authors: G
authors: G
authors: Yu
authors: W
authors: W
authors: Wang
authors: A F
authors: AF
authors: Kluge
authors: P
authors: P
authors: Wendler
authors: P
authors: P
authors: Gallant
mesh_terms: 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*
chemical_list: D004791:Enzyme Inhibitors; D013844:Thiazoles; D000604:Amino Acyl-tRNA Synthetases