OXAMAZIN ANTIBIOTICS

摘要

Disclosed herein are oxamazin monobactam compounds and their use as antibiotics resistant to degradation by β-lactamases. Also disclosed are pharmaceutical compositions containing the compounds and methods of synthesis.

主权项

1. A compound having the structure of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 are independently selected from the group consisting of H, halide, CN, C1-3 alkyl, —X(C1-3 alkyl), —(C1-3 alkyl)OH, —(C1-3 alkyl)CN and C1-3 haloalkyl, or alternatively R1 and R2 together with the atom to which they are attached form a three to four membered carbocyclic ring optionally substituted with one or more halide, or a four membered heterocyclic ring; R3 and R4 are independently selected from the group consisting of halide, CN, C1-3 alkyl, —X(C1-3 alkyl), —X(C1-3 haloalkyl), —(C1-3 alkyl)OH, —(C1-3 alkyl)CN and C1-3 haloalkyl, or alternatively R3 and R4 together with the atom to which they are attached form a three to four membered carbocyclic ring optionally substituted with one or more halide, or a four membered heterocyclic ring; R5 and R6 are independently selected from the group consisting of H, halide, CN, C1-3 alkyl, —X(C1-3 alkyl), —X(C1-3 haloalkyl), —(C1-3 alkyl)OH, —(C1-3 alkyl)CN and C1-3 haloalkyl, or alternatively R5 and R6 together with the atom to which they are attached form a three to four membered carbocyclic ring optionally substituted with one or more halide, or a four membered heterocyclic ring; A is selected from the group consisting of C—H, C-halide, and N; and each X is independently selected from O or S.