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In Vitro and In Vivo Evaluation of an Adamantyl-Based Phenyl Sulfonyl Acetamide against Cutaneous Leishmaniasis Models of Leishmania amazonensis

Authors :
Natália Lins da Silva-Gomes
Ifedayo Victor Ogungbe
Marcos Meuser Batista
Kelly Cristina Demarque
Camila Cardoso Santos
Huaisheng Zhang
Gabriel Melo de Oliveira
Otacilio C. Moreira
Maria de Nazaré Correia Soeiro
Source :
Antimicrob Agents Chemother
Publication Year :
2020
Publisher :
American Society for Microbiology, 2020.

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 [IC 50 ] = 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.

Details

Language :
English
Database :
OpenAIRE
Journal :
Antimicrob Agents Chemother
Accession number :
edsair.doi.dedup.....4a64603b375d48d544e12e72b0bca773