In:
PLOS ONE, Public Library of Science (PLoS), Vol. 17, No. 6 ( 2022-6-6), p. e0269447-
Abstract:
Leishmaniasis is a public health issue. It is among the top five parasitic illnesses worldwide and is one of the most neglected diseases. The current treatment disease includes limitations of toxicity, variable efficacy, high costs and inconvenient doses and treatment schedules. LASSBio-1736 was described as antileishmanial drug-candidate to cutaneous leishmaniasis, displaying plasma stability and with no preliminary signals of hepatic or renal toxicity. In this paper, we described the in vitro pharmacokinetic study of LASSBio-1491 (a less lipophilic isostere of LASSBio-1736) and it is in vitro and in vivo leishmanicidal activities. Our results demonstrated that LASSBio-1491 has high permeability, satisfactory aqueous solubility, long plasma and microsomal half-lives and low in vitro systemic clearance, suggesting a pharmacokinetic profile suitable for its use in a single daily dose. The antileishmanial effect of LASSBio-1491 was confirmed in vitro and in vivo . It exhibited no cytotoxic effect to mammalian cells and displayed good in –vivo effect against BALB/c mice infected with Leishmania major LV39 substrain, being 3 times more efficient than glucantime.
Type of Medium:
Online Resource
ISSN:
1932-6203
DOI:
10.1371/journal.pone.0269447
DOI:
10.1371/journal.pone.0269447.g001
DOI:
10.1371/journal.pone.0269447.g002
DOI:
10.1371/journal.pone.0269447.g003
DOI:
10.1371/journal.pone.0269447.g004
DOI:
10.1371/journal.pone.0269447.t001
DOI:
10.1371/journal.pone.0269447.t002
DOI:
10.1371/journal.pone.0269447.t003
DOI:
10.1371/journal.pone.0269447.t004
DOI:
10.1371/journal.pone.0269447.t005
DOI:
10.1371/journal.pone.0269447.s001
DOI:
10.1371/journal.pone.0269447.s002
DOI:
10.1371/journal.pone.0269447.s003
DOI:
10.1371/journal.pone.0269447.s004
DOI:
10.1371/journal.pone.0269447.s005
DOI:
10.1371/journal.pone.0269447.s006
DOI:
10.1371/journal.pone.0269447.s007
Language:
English
Publisher:
Public Library of Science (PLoS)
Publication Date:
2022
detail.hit.zdb_id:
2267670-3
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