SPECTINAMIDES AS ANTI-TUBERCULOSIS AGENTS

摘要

Novel 3′-deoxy-3′-acylaminospectinomycin compounds are described. Also described are methods of using the 3′-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.

主权项

1. A method of treating a bacterial infection in a subject in need of treatment thereof, the method comprising administering to the subject an effective amount of a compound of Formula (I):wherein:
R1 and R2 are each independently H, alkoxycarbonyl, or aralkoxycarbonyl; R3 is alkyl; R4 is H, hydroxy, alkyl, or alkoxy; and R5 is —C(═O)R6, wherein R6 is: (a) selected from the group consisting of —CH2NHC(CH3)3, —CH(NH2)CH(CH3)CH2CH3, —CH(NH2)CH(CH3)2, —CH(CH2C6H5)NHC(═O)CH2NH2, —CH2CH2NHC(═O)C6H5, and —CH2CH2NHC(═O)CH2C6H5; or (b) selected from the group consisting of heteroaryl, substituted heteroaryl, 2-substituted phenyl, 4-halo-substituted phenyl, —CH2R7, and —C(R8)2; wherein R7 is selected from the group consisting of aralkyl, substituted aralkyl, heteroaryl, substituted heteroaryl, and substituted phenyl, wherein said substituted phenyl is selected from the group consisting of fluoro-substituted phenyl, alkyl-substituted phenyl, 2-substituted phenyl, 3-mono-substituted phenyl, 2,3-di-substituted phenyl, and di-substituted phenyl wherein two phenyl carbons are together substituted with an alkylene; and each R8 is independently aryl or substituted aryl;or a pharmaceutically acceptable salt thereof.