A Study Of Antituberculosis Activities And Crystal Structures Of (E)-2-[2-(Arylidene)Hydrazinyl]Pyrimidine And (E)-N-1 -(Arylidene)Pyrimidine-2-Carbohydrazide Derivatives

A study of the anti-tuberculosis activity against Mycobacterium tuberculosis ATTC 27294 and an X-ray structural determination of (E)-242-(arylidene)hydrazinylipyrimidine, 1, and (E)-N-1-(arylidene)pyrimicline-2-carbohydazide, 2, derivatives are presented. The effect of the substituents in the aryl moiety on the antituberculosis (anti-TB) activities of 1 and 2 is compared with that of other heteroaryl hydrazonyl and acylhydrazonyl derivatives. The biological activities of 1 do not depend on the coordinating ability of the substituted aryl group: in 2, the most effective aryl group is 5-nitrofuranyl. The structure determinations of (E)-2((2-(pyrimidin-2-yOhydrazono)methyl)-phenol, (E)-N'-(2,5-dihydroxybenzylidene)pyrimidine-2-carbohydrazide and of the hydrate of (E)-N'-(2-hydroxy-4-methylbenzylidene) pyrimidine-2-carbohydrazide, and a literature search of related structures in the CCDC data base, allowed an examination of the more important interactions, including the occurrence of X-Y...pi interactions.