| Literature DB >> 32928731 |
Camila C Santos1, Huaisheng Zhang2, Marcos M Batista1, Gabriel M de Oliveira1, Kelly C Demarque1, Natália L da Silva-Gomes3, Otacílio C Moreira3, Ifedayo Victor Ogungbe4, Maria de Nazaré C Soeiro5.
Abstract
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 μM) 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.Entities:
Keywords: adamantyl; cutaneous leishmaniasis; experimental chemotherapy; phenyl sulfonyl acetamide
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Year: 2020 PMID: 32928731 PMCID: PMC7674027 DOI: 10.1128/AAC.01188-20
Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN: 0066-4804 Impact factor: 5.191