An efficient Synthesis of antischistosomal drug Praziquantel and analogues was achieved and the synthetic route designed was to afford structurally diverse analogues for better structureactivity 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-beta-carboline analogues exhibited modearate activity against adult Schistosomamansoni. Tetrahydro-beta-carboline analogues showed moderate activity whereas the presence of p-trifluoromethylbenzoyl and p-toluenesulphonyl moieties resulted in complete suppression of antischistosomal activity.
Synthesis of new Praziquantel analogues: Potential candidates for the treatment of schistosomiasis
2012
Abstract
An efficient Synthesis of antischistosomal drug Praziquantel and analogues was achieved and the synthetic route designed was to afford structurally diverse analogues for better structureactivity 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-beta-carboline analogues exhibited modearate activity against adult Schistosomamansoni. Tetrahydro-beta-carboline analogues showed moderate activity whereas the presence of p-trifluoromethylbenzoyl and p-toluenesulphonyl moieties resulted in complete suppression of antischistosomal activity.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
