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An efficient synthesis of antischistosomal drug praziquantel and analogues was achieved and the synthetic route designed was to afford structurally diverse analogues for better structure-activity relationship understanding. Total of nineteen PZQ analogues with structural variations at amide, piperazine and aromatic moieties have been synthesized and fully characterized. Among all the new analogues tested for antischistosomal activity, one dimethoxy tetrahydroisoquinoline analogue and two tetrahydro-β-carboline analogues exhibited moderate activity against adult Schistosoma mansoni. Tetrahydro-β-carboline analogues showed moderate activity whereas the presence of p-trifluoromethylbenzoyl and p-toluenesulphonyl moieties resulted in complete suppression of antischistosomal activity. Copyright © 2011 Elsevier Ltd. All rights reserved.

Citation

Partha Sarathi Sadhu, Singam Naveen Kumar, Malapaka Chandrasekharam, Livia Pica-Mattoccia, Donato Cioli, Vaidya Jayathirtha Rao. Synthesis of new praziquantel analogues: potential candidates for the treatment of schistosomiasis. Bioorganic & medicinal chemistry letters. 2012 Jan 15;22(2):1103-6

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PMID: 22217873

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