Design, synthesis and biological evaluation of imidazo[1,2-a]pyridine analogues or derivatives as anti-helmintic drug.

Abstract

The Albendazole was used as the lead compound, which was modified by structural transformation and with alkyl groups. A total of 18 compounds (4a-4r) were designed and synthesized. The in vitro experiment results showed that compounds 4e, 4f, 4k, 4l, 4q and 4r had good inhibitory effect on egg and imago of roundworm. IC50 of compound 4l to anti-egg of roundworm was 0.65±0.01μmol/L and to anti-imago of roundworm was 1.04±0.01μmol/L. At the same time, it showed that compound 4l had the best effect in vivo, and the rate of anti-helmintic could reach more than 99%. The results of acute toxicity tests indicated that these compounds were with LD50 > 2100 mg/kg by oral administration, so they were low toxicity compounds. In a word, compound 4l was most likely to be a new anti-helmintic drug through screening in vitro and in vivo.