NITROHETEROARYL-CONTAINING RIFAMYCIN DERIVATIVES

摘要

Substituted rifamycin derivatives of formula I uses thereof and pharmaceutical compositions containing the rifamycin derivatives are disclosed. Methods of synthesizing these substituted rifamycin derivatives are also disclosed. The rifamycin derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.or their pharmaceutically acceptable salt thereof, wherein R₁ is a hydrogen or acetyl group, G is a structure of formula (II, III, IV or V): wherein, in formula (II, III, IV or V), Q is N- or CR₂. which is bonded to a linkage, group "L", which in turn is bonded to a structure A-NO²,and R₂ is a group selected from hydrogen, substituted or unsubstituted (C₁-C₆)alkyl, aryl, heteroaryl, or heterocycloalkyl group; The structure A-NO² is a structural formula (VI1 VII, VIII or IX): wherein Y is a bond which is bonded to linkage group "L", defined as above; and Z is a carbon (-CR₇R₈-), carbonyl (-C(O)-), amide (-C(O)N-), sulfonamide (-S(O₂)N-), or a heteroatom selected from N, O, S, SO or SO₂; wherein R₅, R₆, R₇, and R₈ are independently a group selected from hydrogen, substituted or unsubstituted (C₁-C₆)alkyl, aryl. heteroaryl. or heterocycloalkyl group; R₅ and R₆ R₇ and R₈ can join together to form a five to seven-member ring system optionally containing one to three heteroatoms.