In vitro and in vivo evaluation of an adamantyl-based phenyl sulfonyl acetamide against cutaneous leishmaniasis models of L. amazonensis.
2020
Phenotypic assay against L. amazonensis in vitro and in vivo led to identification of an adamantyl-based phenyl sulfonyl acetamide (1) as a promising antileishmanial agent. Compound 1 inhibited the growth of intracellular forms of L. amazonensis (IC50 4 μM), exhibited low toxicity to host cells, with selectivity index >125. However, in cutaneous leishmaniasis mouse model, 1 did not reduce lesions and parasite load when administered as monotherapy or given simultaneously with suboptimal dose of miltefosine.
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