BENZOXABOROLE COMPOUNDS AND USES THEREOF

摘要

Norvaline and/or other amino acids that are capable of being acylated onto tRNALeu by LeuRS, in combination with substituted benzoxaboroles, such as a compound having a structure according to formula III:;;and methods for decreasing the frequency of resistance and/or reducing the rate of resistance and/or suppressing the emergence of resistance that develops in bacteria exposed to a substituted benzoxaborole or salt thereof by administering a combination of a substituted benzoxaborole such as a compound of formula III or salt thereof and an amino acid or a salt thereof.

主权项

1. A combination of an amino acid or amino acid salt that is capable of being acylated onto tRNALeu by LeuRS and a compound having a structure according to formula II: wherein R3 is a member selected from H, cyano, substituted or unsubstituted nitroalkyl and substituted or unsubstituted aminoalkyl; Ra is a member selected from H and —YR5; wherein Y is a member selected from O and S; R5 is a member selected from H, substituted or unsubstituted alkyl and substituted or unsubstituted heteroalkyl with the proviso that Ra and R3 cannot both be H; and with the proviso that when R3 is H, Ra does not have a structure which is a member selected from: unsubstituted benzyloxy, —OCH2COOH, methoxy, ethoxy, with the proviso that when Ra is H, R3 is not cyano, or a salt thereof.