Structure-Property Optimization of a Series of Imidazopyridines for Visceral Leishmaniasis.
ACS Infect Dis
; 9(8): 1470-1487, 2023 08 11.
Article
em En
| MEDLINE
| ID: mdl-37417544
ABSTRACT
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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Leishmaniose
/
Leishmania
/
Leishmaniose Visceral
Limite:
Humans
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article