Antileishmanial activity of new hybrid tetrahydroquinoline and quinoline derivatives with phosphorus substituents.
DNA-Topoisomerase
Leishmania
Phosphorus substituted quinoline derivatives
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
15 Jan 2019
15 Jan 2019
Historique:
received:
24
09
2018
revised:
24
10
2018
accepted:
29
10
2018
pubmed:
9
11
2018
medline:
5
2
2019
entrez:
9
11
2018
Statut:
ppublish
Résumé
Heterocyclic compounds, such as hybrid tetrahydroquinoline and quinoline derivatives with phosphorated groups, have been prepared by multicomponent cycloaddition reaction between phosphorus-substituted anilines, aldehydes and styrenes. The antileishmanial activity of these compounds has been evaluated on both promastigotes and intramacrophagic amastigotes of Leishmania infantum. Good antileishmanial activity of functionalized tetrahydroquinolines 4a, 5a, 6b and quinoline 8b has been observed with similar activity than the standard drug amphotericin B and close selective index (SI between 43 and 57) towards L. infantum amastigotes to amphotericin B. Special interest shows tetrahydroquinolylphosphine sulfide 5a with an EC
Identifiants
pubmed: 30408746
pii: S0223-5234(18)30942-5
doi: 10.1016/j.ejmech.2018.10.065
pii:
doi:
Substances chimiques
Antiprotozoal Agents
0
Quinolines
0
Phosphorus
27YLU75U4W
1,2,3,4-tetrahydroquinoline
CCR50N1Z9G
DNA Topoisomerases, Type I
EC 5.99.1.2
TOP1 protein, human
EC 5.99.1.2
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
18-31Informations de copyright
Copyright © 2018 Elsevier Masson SAS. All rights reserved.