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- W4319216391 abstract "For the Schistosoma mansoni flatworm pathogen, we report a structure-activity relationship of 25 derivatives of the N-phenylbenzamide compound, 1 (MMV687807), a Medicines for Malaria Venture compound for which bioactivity was originally identified in 2018. Synthesized compounds were cross-screened against the HEK 293 mammalian cells. Compounds 9 and 11 were identified as fast-acting schistosomicidal compounds whereby adult worm integrity was severely compromised within 1 h. Against HEK 293 mammalian cells, both compounds exhibited high CC50 values (9.8 ± 1.6 and 11.1 ± 0.2 µM respectively) which could translate to comfortable selectivity. When evaluated in a concentration-response format, compound 9 was active in the nanomolar range (EC50 = 80 nM), translating to a selectivity index of 123 over HEK 293 cells. The data encourage the further investigation of N-phenylbenzamides as antischistosomals." @default.
- W4319216391 created "2023-02-05" @default.
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- W4319216391 date "2023-02-01" @default.
- W4319216391 modified "2023-10-11" @default.
- W4319216391 title "Activity of N-phenylbenzamide analogs against the neglected disease pathogen, Schistosoma mansoni" @default.
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- W4319216391 doi "https://doi.org/10.1016/j.bmcl.2023.129164" @default.
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