Antibacterial agents: sidechainfluorinated myxopyronin derivatives

摘要

The invention provides compounds of Formula I:;
and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and G are as described in the specification, as well as compositions comprising a compound of formula I, methods of making such compounds, and methods of using such compounds, e.g., as inhibitors of bacterial RNA polymerase and as antibacterial agents.

主权项

1. A compound of formula I:or a salt thereof, wherein:
R1 is one of CF3, CHF2, and CH2F; R2 is absent or is C1-C8 alkyl, optionally substituted with halo; R3, R4, and R5 are independently H or methyl; G is one of —CH═CH—NHC(O)—R6, —CH═CH—NHC(S)—R6, —CH2CH2NHC(O)—R6, —CH2CH2NHC(S)—R6, —CH2NHNHC(O)—R6, or —CH2NHNHC(S)—R6; R6 is one of C1-C6 alkyl, —O(C1-C6 alkyl), —S(C1-C6 alkyl), or —N(R7)2; and each R7 is independently H or —C1-C6 alkyl.