Abstract
A series of 5-(aryl substituted)-5-(benzylideneamino) -1H- 1, 2, 4-triazole-3-thiol derivatives were synthesized by condensation of oxazol-5-ones by reaction of Hippuric acid and different aldehydes with thiosemicarbazide. Structures of the compounds were characterized on the basis of IR, C13NMR and H1 NMR. Compounds 1b-12b was screened for antihelmintic activity. Test results revealed that compound 7b and 10b showed high potency with paralysis time of 3.3 and 3.1 min and death time of 4.1 and 4.5 min when compared with the standard drug albendazole with paralysis time of 11 min and death time of 21min, respectively, at the same concentration of 50mg/ml. All compounds were found to posses both antihelmintic properties. The derivatives were also evaluated by Insilco methods predicting that the synthesised compounds exbhit drug like properties,have good enzyme inhibition activities with teratogenic effects providing an approach to develop new potent antihelmintic prototypes for further optimization and development to get new leads in the treatment of helminth infestations.
