期刊
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
卷 64, 期 12, 页码 -出版社
AMER SOC MICROBIOLOGY
DOI: 10.1128/AAC.01188-20
关键词
cutaneous leishmaniasis; adamantyl; phenyl sulfonyl acetamide; experimental chemotherapy
资金
- Fortalecimento dos Programas de Gestao Estrategica de Pesquisa da Fiocruz Rede de Plataformas Fiocruz [VPPLR-001-Fio-14]
- Fundacao Carlos Chagas Filho de Amparo a Pesquisa do Estado do Rio de Janeiro (FAPERJ)
- Conselho Nacional Desenvolvimento cientifico e Tecnologico (CNPq)
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES)
- Fundacao Oswaldo Cruz, PAEF/CNPq/Fiocruz
- U.S. National Institutes of Health [SC3GM122629, G12MD007581]
Phenotypic assay against Leishmania amazonensis in vitro and in vivo led to identification of an adamantyl-based phenyl sulfonyl acetamide (compound 1) as a promising antileishmanial agent. Compound 1 inhibited the growth of intracellular forms of L. amazonensis (50% inhibitory concentration [IC50] = 4 mu M) and exhibited low toxicity to host cells, with a selectivity index (SI) of >125. However, in a cutaneous leishmaniasis (CL) mouse model, compound 1 did not reduce lesions and parasite load when administered as monotherapy or when given simultaneously with a suboptimal dose of miltefosine.
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