Antischistosomal Ozonide Glycine Ethyl Esters.

Building on the discovery that synthetic ozonides have not only antimalarial but also antischistosomal properties, we now report the synthesis and antischistosomal activity of a series of ozonide glycine ethyl esters. We identified ozonide glycine zwitterion 19 and its ethyl ester 17 as new antischistosomal lead compounds. Ozonides 17 and 19 had high in vivo antischistosomal activity against adult worms and low cytotoxicity. Based on C max and AUC0-24 h values, exposure of 19 after administration of its ethyl ester 17 was approximately 1.5-fold higher than that observed after dosing 19 itself.