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In Vitro and In Vivo Evaluation of an Adamantyl-Based Phenyl Sulfonyl Acetamide against Cutaneous Leishmaniasis Models of Leishmania amazonensis
- 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.
- Subjects :
- Pharmacology
Sulfonyl
chemistry.chemical_classification
0303 health sciences
Miltefosine
030306 microbiology
medicine.disease
Parasite load
In vitro
03 medical and health sciences
chemistry.chemical_compound
Infectious Diseases
Cutaneous leishmaniasis
chemistry
In vivo
medicine
Pharmacology (medical)
Experimental Therapeutics
IC50
Acetamide
030304 developmental biology
medicine.drug
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- Antimicrob Agents Chemother
- Accession number :
- edsair.doi.dedup.....4a64603b375d48d544e12e72b0bca773