Benzazol-Derivate und Verfahren zur Herstellung derselben

摘要

1,234,058. Pyridylalkyl - oxo or -thio azole derivatives. EGYSULT GYOGYSZER ES TAPSZERGYAR. 21 Oct., 1968, No. 49798/68. Heading C2C. Novel compounds having the general Formula I wherein A is an alkylene group of 1-5 carbon atoms or a valence bond; X is an -NH group, an oxygen or sulphur atom; Y is a sulphur or oxygen atom; Z is a -CH- group or a nitrogen atom; R 1 is a hydrogen atom or a methyl group; R 2 is a hydrogen or chlorine atom, or a -NO 2 or -CH 3 group; and n is an integer from I to 3; and their acid addition salts and quaternary ammonium derivatives are prepared by reacting a compound having the general Formula II wherein A, R 1 , R 2 , X, Y and Z are as above, with a pyridine derivative of Formula III wherein B is an -NH 2 group or a halogen atom and n is as above, or with a salt thereof; and, if desired, transforming the obtained product to a pharmaceutically acceptable acid addition salt or a quaternary ammonium derivative. Preferably, where B stands for an -NH 2 group the reaction is carried out at a temperature of from 100-150‹ C., and when B is a halogen atom, the reaction is carried out in the presence of an acid-binding agent such as sodium hydroxide. The compounds of the invention have tuberculostatic, other bacteriostatic, insecticidal, fungicidal, antiviral, anthelmitic and antiinflammatory activity, and may be used in pharmaceutical compositions in combination with a carrier, for example in forms suitable for oral, parenteral or rectal administration.