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The drug arsenal available for the treatment of these diseases is limited; for example, praziquantel is the only drug currently used to treat \u2265240 million people each year infected with <jats:italic>Schistosoma spp<\/jats:italic>., and there is justified concern about the emergence of drug resistance. In this study, we screened biarylalkyl carboxylic acid derivatives for their antischistosomal activity against <jats:italic>S.\u2005mansoni<\/jats:italic>. These compounds showed significant influence on egg production, pairing stability, and vitality. Tegumental lesions or gut dilatation was also observed. Substitution of the terminal phenyl residue in the biaryl scaffold with a 3\u2010hydroxy moiety and derivatization of the terminal carboxylic acid scaffold with carboxamides yielded compounds that displayed significant antischistosomal activity at concentrations as low as 10\u2005\u03bc<jats:sc>m<\/jats:sc> with satisfying cytotoxicity values. 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