Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 3, Pages 258-265Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00455
Keywords
Schistosomiasis; Schistosoma spp; Target class repurposing; Neglected tropical disease; Parasite-hopping
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Funding
- National Institutes of Health [R01AI082577, R56AI099476, R01AI124046, R21AI127594, R01AI126311, R01AI114685]
- National Research Foundation of South Africa
- NIH-NIAID [R21AI126296, OPP1171488, HHSN272201700014I]
- Bill and Melinda Gates Foundation
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We recently reported a series of compounds for a solubility-driven optimization campaign of antitrypanosomal compounds. Extending a parasite-hopping approach to the series, a subset of compounds from this library has been cross-screened for activity against the metazoan flatworm parasite, Schistosoma mansoni. This study reports the identification and preliminary development of several potently bioactive compounds against adult schistosomes, one or more of which represent promising leads for further assessment and optimization.
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