| Summary: | This work describes the synthesis of quinoline-based <i>N</i>--heterocyclic arenes and their biological evaluation as molluscicides against adult <i>Biomophalaria alexandrina</i> snails as well as larvicides against <i>Schistosoma mansoni</i> larvae (miracidia and cercariae). Molecular docking studies were demonstrated to investigate their affinity for cysteine protease protein as an interesting target for antiparasitics. Compound <b>AEAN</b> showed the best docking results followed by <b>APAN</b> in comparison to the co-crystallized ligand D1R reflected by their binding affinities and RMSD values. The egg production, hatchability of <i>B. alexandrina</i> snails and ultrastructural topography of <i>S. mansoni</i> cercariae using SEM were assessed. Biological evaluations (hatchability and egg-laying capacity) revealed that the quinoline hydrochloride salt <b>CAAQ</b> was the most effective compound against adult <i>B. alexandrina</i> snails, whereas the indolo-quinoline derivative <b>APAN</b> had the most efficiency against miracidia, and the acridinyl derivative <b>AEAA</b> was the most effective against cercariae and caused 100% mortality. <b>CAAQ</b> and <b>AEAA</b> were found to modulate the biological responses of <i>B. alexandrina</i> snails with/without <i>S. mansoni</i> infection and larval stages that will affect <i>S. mansoni</i> infection. <b>AEAA</b> caused deleterious morphological effects on cercariae. <b>CAAQ</b> caused inhibition in the number of eggs/snail/week and reduced reproductive rate to 43.8% in all the experimental groups. <b>CAAQ</b> and <b>AEAA</b> can be recommended as an effective molluscicide of plant origin for the control program of schistosomiasis.
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