Publications by authors named "Joy U Laydbak"
Chagas disease, caused by the protozoan pathogen Trypanosoma cruzi, remains a challenging infection due to the unavailability of safe and efficacious drugs. Inhibitors of the trypanosome sterol 14α-demethylase enzyme (CYP51), including azole antifungal drugs, are promising candidates for development as anti-Chagas disease drugs. Posaconazole is under clinical investigation for Chagas disease, although the high cost of this drug may limit its widespread use.
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- - A series of urea-based inhibitors targeting methionyl-tRNA synthetase were developed to combat human African trypanosomiasis (HAT), showing high selectivity for the parasite's enzyme.
- - These compounds demonstrated effective inhibition of parasite growth with concentrations as low as 0.15 μM, while maintaining low toxicity towards mammalian cells.
- - Some compounds exhibited good absorption and penetration into the central nervous system in mice, indicating potential for oral administration, though further optimization is needed to enhance their efficacy against the parasite.