In Vitro and In Vivo Evaluation of an Adamantyl-Based Phenyl Sulfonyl Acetamide against Cutaneous Leishmaniasis Models of Leishmania amazonensis
| Autor: | 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 |
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| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
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 |
| Zdroj: | Antimicrob Agents Chemother |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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