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ACS Infect Dis ; 9(8): 1470-1487, 2023 08 11.
Artículo en Inglés | MEDLINE | ID: mdl-37417544

RESUMEN

Leishmaniasis is a collection of diseases caused by more than 20 Leishmania parasite species that manifest as either visceral, cutaneous, or mucocutaneous leishmaniasis. Despite the significant mortality and morbidity associated with leishmaniasis, it remains a neglected tropical disease. Existing treatments have variable efficacy, significant toxicity, rising resistance, and limited oral bioavailability, which necessitates the development of novel and affordable therapeutics. Here, we report on the continued optimization of a series of imidazopyridines for visceral leishmaniasis and a scaffold hop to a series of substituted 2-(pyridin-2-yl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazoles with improved absorption, distribution, metabolism, and elimination properties.


Asunto(s)
Leishmania , Leishmaniasis Visceral , Leishmaniasis , Humanos , Leishmaniasis Visceral/tratamiento farmacológico , Enfermedades Desatendidas , Imidazoles/farmacología
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