BIS-CATIONIC HETEROAROMATICS AS MACROFILARICIDES - SYNTHESIS OF BIS-AMIDINE AND BIS-GUANYLHYDRAZONE DERIVATIVES OF SUBSTITUTED IMIDAZIO[1,2-A] PYRIDINES

A series of guanylhydrazone, amidine, and hydrazone derivatives of 2-p henylimidazo[1,2-a]pyridine have been prepared and evaluated for macro filarial activity against Acanthocheilonema viteae and Brugia pahangi in jirds. Compounds with 4',6-bis-substitution by cyclic guanylhydrazo ne groups show activity. 4',6-Bis-amidines show some activity but are more toxic; 4'- or 6-monosubstituted compounds are inactive. 2,6-Bis-s ubstituted compounds lacking the phenyl ring are inactive. 4',6-Bis-su bstituted compounds having additional double bonds inserted between th e heterocyclic ring and the phenyl ring or between the substituent and the ring system show reduced activity.