SYNTHESIS AND ANTINOCICEPTIVE PROPERTIES OF NEW STRUCTURALLY PLANNED IMIDAZO[1,2-A]PYRIDINE 3-ACYLARYLHYDRAZONE DERIVATIVES

This paper describes recent results of a research program aiming at th e synthesis and pharmacological evaluation of new N-heterocyclic funct ionalized acylarylhydrazone compounds, belonging to 3 l-(2-methyl-imid azo[1,2-a]pyridinyl)-arylhydrazone 2 series. These compounds were stru cturally planned applying classical ring bioisosterism strategies on p reviously described 4-acyl-(N-phenylpyrazolyl)-arylhydrazone, which pr esented important analgesic properties, in order to identify the pharm acophore contribution of the acylarylhydrazone moiety and investigate the structure-activity relationship (SAR) in these series. The results herein disclosed indicate that this strategy of molecular modificatio n gave rise to a new series of analgesic and anti-inflammatory agents, where the activity seems to be more dependent on the nature of the pa ra-substituent at the pharmacophore acylarylhydrazone (AAH) moiety, th an the N-heterocyclic acyl-ring pattern. (C) Elsevier, Paris.