In Vitro And In Vivo Evaluation Of An Adamantyl-Based Phenyl Sulfonyl Acetamide Against Cutaneous Leishmaniasis Models Of Leishmania Amazonensis
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY(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 [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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Key words
cutaneous leishmaniasis, adamantyl, phenyl sulfonyl acetamide, experimental chemotherapy
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