title: Comparative in vitro activities of GSK2251052, a novel boron-containing leucyl-tRNA synthetase inhibitor, against 916 anaerobic organisms.
abstract: We studied the comparative in vitro activity of GSK2251052, a novel boron leucyl-tRNA synthetase inhibitor, against 916 clinical anaerobic isolates using CLSI methods. The GSK MIC50/MIC90 for all isolates tested were 2 and 4 μg/ml, and the MIC90s against 302 Bacteroides fragilis and Bacteroides thetaiotaomicron strains were 4 and 8 μg/ml, respectively. All Clostridium perfringens strains had GSK2251052 MICs of >32 μg/ml. There was no relationship between increased MICs for any other antibiotics and that of GSK2251052.
authors: RM Alden Research Laboratory, Culver City, California, USA. ejcgmd@aol.com
authors: Ellie J C
authors: EJ
authors: Goldstein
authors: Diane M
authors: DM
authors: Citron
authors: Kerin L
authors: KL
authors: Tyrrell
authors: C Vreni
authors: CV
authors: Merriam
mesh_terms: D000693:Anaerobiosis; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D001439:Bacteroides / Q000187:drug effects* / Q000201:enzymology / Q000254:growth & development / Q000302:isolation & purification; D001441:Bacteroides fragilis / Q000187:drug effects* / Q000201:enzymology / Q000254:growth & development / Q000302:isolation & purification; D001896:Boron Compounds / Q000494:pharmacology*; D003016:Clostridium perfringens / Q000187:drug effects* / Q000201:enzymology / Q000254:growth & development / Q000302:isolation & purification; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007935:Leucine-tRNA Ligase / Q000037:antagonists & inhibitors / Q000378:metabolism; D008826:Microbial Sensitivity Tests
chemical_list: C583949:3-(aminomethyl)-7-(3-hydroxypropoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole; D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D001896:Boron Compounds; D004791:Enzyme Inhibitors; D007935:Leucine-tRNA Ligase