Novel hydrazone derivatives of N-amino-11-azaartemisinin with high order of antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in Swiss mice via intramuscular route.
11-azaartemisnin
Antimalarial Activity
Artemisinin
Multidrug-Resistant
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 02 2022
15 02 2022
Historique:
received:
11
10
2021
revised:
23
12
2021
accepted:
26
12
2021
pubmed:
3
1
2022
medline:
17
2
2022
entrez:
2
1
2022
Statut:
ppublish
Résumé
Novel hydrazone derivatives 10a-m were prepared from N-Amino-11-azaartemisinin (9) and screened for their antimalarial activity by oral and intramuscular (i.m.) routes against multidrug-resistant Plasmodium yoelii in Swiss mice model. Several of the hydrazone derivatives showed higher order of antimalarial activity. Compounds 10b, 10g, 10m provided 100% protection to the infected mice at the dose of 24 mg/kg × 4 days via oral route. Fluorenone based hydrazone 10m the most active compound of the series, provided 100% protection at the dose of 6 mg/kg × 4 days via intramuscular route and also provided 100% protection at the dose of 12 mg/kg × 4 days via oral route. While artemisinin gave 100% protection at 48 mg/kg × 4 days and only 60% protection at 24 mg/kg × 4 days via intramuscular (i.m.) route. Compound 10m found to be four-fold more active than artemisinin via intramuscular route.
Identifiants
pubmed: 34974111
pii: S0960-894X(21)00749-6
doi: 10.1016/j.bmcl.2021.128522
pii:
doi:
Substances chimiques
Antimalarials
0
Artemisinins
0
Hydrazones
0
artemisinin
9RMU91N5K2
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
128522Informations de copyright
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