Abstract
In the present invention, there are disclosed substituted diazoles of the 1,3,4-oxadiazole and 1,3,4-thiadiazole group, of the general formula I wherein X denotes O or S; R is selected from the group consisting of: H, -NH2, alkyl containing 1 to 11 carbon atoms, cyclohexyl-, benzyl-, phenyl-, pyridyl- or phenyl- substituted in positions 2, 3, 4 and 5, by one or more electron-acceptor groups comprising -NO2, -N(alkyl)3, -CF3, CCl3, -CN, -COOH, -COOAlk, -COOAr, -CHO, -COAlk, -COAr, -F, -CI, -Br, -I, and/or by one or more electron-donor groups comprising -NH2, -NHalkyl, -N(alkyl)2, -OH, -Oalkyl, -Oaryl, -NHCOCH3, -NHCOalkyl; -NHCOaryl; -alkyl, -aryl, wherein when R1 and R3 is -NO2, then R2 and R4 is -H, or when R1 and R3 is -H, then R2 and R4 is -NO2. These compounds can be prepared by easy syntheses and have low toxicity and significant activity against mycobacteria including their multiresistant strains.
The invention provides also a pharmaceutical composition having substituted diazole of the general formula I as the active substance, as well as the use of this substituted diazole as antituberculosis agent.