In:
PLOS ONE, Public Library of Science (PLoS), Vol. 16, No. 11 ( 2021-11-1), p. e0259008-
Abstract:
Leishmaniasis is a neglected disease that affects 12 million people living mainly in developing countries. Herein, 24 new N -oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antileishmanial activity. Compound 4f , a furoxan derivative, was particularly remarkable in this regard, with EC 50 value of 3.6 μM against L . infantum amastigote forms and CC 50 value superior to 500 μM against murine peritoneal macrophages. In vitro studies suggested that 4f may act by a dual effect, by releasing nitric oxide after biotransformation and by inhibiting cysteine protease CPB (IC 50 : 4.5 μM). In vivo studies using an acute model of infection showed that compound 4f at 7.7 mg/Kg reduced ~90% of parasite burden in the liver and spleen of L . infantum -infected BALB/c mice. Altogether, these outcomes highlight furoxan 4f as a promising compound for further evaluation as an antileishmanial agent.
Type of Medium:
Online Resource
ISSN:
1932-6203
DOI:
10.1371/journal.pone.0259008
DOI:
10.1371/journal.pone.0259008.g001
DOI:
10.1371/journal.pone.0259008.g002
DOI:
10.1371/journal.pone.0259008.g003
DOI:
10.1371/journal.pone.0259008.g004
DOI:
10.1371/journal.pone.0259008.g005
DOI:
10.1371/journal.pone.0259008.g006
DOI:
10.1371/journal.pone.0259008.t001
DOI:
10.1371/journal.pone.0259008.t002
DOI:
10.1371/journal.pone.0259008.s001
DOI:
10.1371/journal.pone.0259008.s002
DOI:
10.1371/journal.pone.0259008.s003
DOI:
10.1371/journal.pone.0259008.s004
DOI:
10.1371/journal.pone.0259008.s005
DOI:
10.1371/journal.pone.0259008.s006
DOI:
10.1371/journal.pone.0259008.r001
DOI:
10.1371/journal.pone.0259008.r002
DOI:
10.1371/journal.pone.0259008.r003
DOI:
10.1371/journal.pone.0259008.r004
Language:
English
Publisher:
Public Library of Science (PLoS)
Publication Date:
2021
detail.hit.zdb_id:
2267670-3
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