Discovery of new organoselenium compounds as antileishmanial agents.
Antiprotozoal Agents
/ chemical synthesis
Cell Survival
/ drug effects
Cells, Cultured
Dose-Response Relationship, Drug
Drug Discovery
Humans
Leishmania infantum
/ drug effects
Leishmaniasis
/ drug therapy
Molecular Structure
Organoselenium Compounds
/ chemical synthesis
Parasitic Sensitivity Tests
Structure-Activity Relationship
THP-1 Cells
Carbonic anhydrase
Inhibitor
Leishmania
Metalloenzymes
Selenium
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
05 2019
05 2019
Historique:
received:
05
10
2018
revised:
13
12
2018
accepted:
30
01
2019
pubmed:
12
2
2019
medline:
14
4
2020
entrez:
12
2
2019
Statut:
ppublish
Résumé
We report new organoselenium compounds bearing the sulfonamide moiety as effective inhibitors of the β-isoform of Carbonic Anhydrase from the unicellular parasitic protozoan L. donovani chagasi. All derivatives were evaluated in vitro for their leishmanicidal activities against Leishmania infantum amastigotes along with their cytotoxicities in human THP-1 cells. Compounds 3e-g showed their activity in the low micromolar range with IC
Identifiants
pubmed: 30743174
pii: S0045-2068(18)31135-0
doi: 10.1016/j.bioorg.2019.01.069
pii:
doi:
Substances chimiques
Antiprotozoal Agents
0
Organoselenium Compounds
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
339-345Informations de copyright
Copyright © 2019 Elsevier Inc. All rights reserved.