Abstract
A novel series of substituted tetrahydropyrimidinediones has been synthesized and evaluated for their schistosomicidal activity both in vitro and in vivo using praziquantel as a therapeutic control. All the tested compounds except compounds (4), (6) and (7a) showed in vitro schistosomicidal activity, however only compound (9) showed in vivo activity in Swiss strain albino mice as evidenced by significant reduction in worm load , tissue egg count , liver granuloma number and size, and histopathological study of the liver. Moreover, electron microscopy scanning of adult S. mansoni recovered from treated animals with compound 9 revealed tegumental changes. These data point to 2-(2,6-dioxo-1,2,3,6- tetahydropyrimidin-4-yl)isoindoline-1,3-dione (9) as a promising new antischistosomal agent.
Keywords: Tetrahydropyrimidinediones, Schistosomicidal activity, Praziquantel
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