Schistosomiasis is a parasitic disease caused by the blood flukes from the genus Schistosoma and is one of the major neglected tropical diseases of the world, second only to malaria. There is no vaccine available and current treatment consists of Praziquantel monotherapy which is refractory to juvenile worms necessitating the need for new drug discovery. The small molecule inhibition of the class I zinc-dependent histone deacetylases is a promising alternative for schistosomiasis therapy. Specifically, SmHDAC8 has been shown to be a validated target as it is essential for worm viability and egg production. We have designed and synthesized 1,2,3,4-tetrahydroisoquinoline hydroxamic acids with low micromolar potency in vitro and isoform selectivity to HDAC8. We hypothesize the activity is due to a chemotype-induced conformational change unique to the HDAC8 isoform.

Novel, potent, and selective inhibitors of SmHDAC8 with schistosomicidal activity

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