Structure-Property Optimization of a Series of Imidazopyridines for Visceral Leishmaniasis

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Dichiara, Maria ; Simpson, Quillon J. ; Quotadamo, Antonio ; Jalani, Hitesh B. ; Huang, Anson X. ; Millard, Caroline C. ; Klug, Dana M. ; Tse, Edwin G. ; Todd, Matthew H. ; Silva, Daniel Gedder ; Emery, Flavio da Silva ; Carlson, J. Eric ; Zheng, Shao-Liang ; Vleminckx, Margot ; Matheeussen, An ; Caljon, Guy ; Pollastri, Michael P. ; Sjo, Peter ; Perry, Benjamin ; Ferrins, Lori

• Tipo de documento: Artigo Científico
• Fonte: ACS INFECTIOUS DISEASES; v. 9, n. 8, p. 18-pg., 2023-07-07.

Resumo

Leishmaniasis is a collection of diseases caused by morethan 20 Leishmania parasite speciesthat manifest as eithervisceral, cutaneous, or mucocutaneous leishmaniasis. Despite the significantmortality and morbidity associated with leishmaniasis, it remainsa 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 imidazopyridinesfor visceral leishmaniasis and a scaffold hop to a series of substituted2-(pyridin-2-yl)-6,7-dihydro-5H-pyrrolo[1,2-a]imidazoles with improved absorption, distribution, metabolism,and elimination properties. (AU)

• Processo FAPESP: 21/11899-0 - Desenvolvimento de uma nova série de compostos heterociclos potentes e seletivos como agentes anti-infecciosos
• Beneficiário: Daniel Gedder Silva
• Modalidade de apoio: Bolsas no Exterior - Estágio de Pesquisa - Pós-Doutorado
• Processo FAPESP: 17/21146-4 - Explorando a química heterocíclica e a epigenética para o desenvolvimento de compostos de interesse químico medicinal
• Beneficiário: Flavio da Silva Emery
• Modalidade de apoio: Auxílio à Pesquisa - Regular