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IN VITRO AND IN VIVO EVALUATION OF AN ADAMANTYL-BASED PHENYL SULFONYL ACETAMIDE AGAINST CUTANEOUS LEISHMANIASIS MODELS OF LEISHMANIA AMAZONENSIS
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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 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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