OXA- AND THIA-DIAZOLES USEFUL IN THE TREATMENT OF TUBERCULOSIS

摘要

A substituted diazole of genera l formula (1) wherein X is 0 or S; R is selected from the group consisting of: H, NH2-, C1-C11n alkyl, cyclohexyl-, benzyl-, phenyl-, pyridyl- or phenyl- substituted, in positions 2, 3, 4 or 5, by one or more electron-acceptor groups comprising -N02, -N(a lkyl)3, -CF3, CC13, -CN, -COOH, -COOAlk, -COOAr, -CHO, -COAlk, -COAr, -F, -CI, -Br, -I, and/or electron-donor groups comprising -NH2, -N Halkyl, -N(alkyl)2, -OH, -Oalkyl, -Oaryl, -NHCOCH3, -NHCOalkyl; -NHCOaryl; -alkyl, -aryl, wherein when R1 and R3 is -N02, then R2 a R4 is -H, or when R1 and R3 is -H, then R2 and R4 is -N02. These compounds can be prepared by easy synthesis and have low toxicity and significant activity against mycobacteria including their multiresistant strains. The invention provides also a pharmaceutical preparation having substituted diazole of formula (I) as the active ingredient, as well as the use of this substituted diazole as antituberculotic.