Journal
CHEMMEDCHEM
Volume 13, Issue 22, Pages 2374-2389Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201800572
Keywords
drug discovery; medicinal chemistry; neglected tropical diseases; praziquantel; schistosomiasis
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Funding
- Deutsche Forschungsgemeinschaft [GR 1549/5-2]
- LOEWE Center DRUID within the Hessian Excellence Initiative
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Chemotherapy based on repeated doses of praziquantel remains the most effective control strategy against schistosomiasis, a neglected tropical disease caused by platyhelminths of the genus Schistosoma spp. Its long-term use, however, raises serious concerns about drug resistance against praziquantel. Therefore, it is generally acknowledged that alternative treatment options are urgently needed. This Review summarizes data on relinquished drugs as well as recent advances in the area of antischistosomal compounds from a medicinal chemistry point of view. Furthermore, insights into the structure-activity relationships of each class of compounds are presented including in vitro and in vivo data, if available. Although many compounds have demonstrated good antischistosomal activity in vitro, they offer little promise to replace praziquantel. Nevertheless, the race to develop novel antischistosomal agents is ongoing.
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