Quinoline carboxamide core moiety-based compounds inhibit P. falciparumfalcipain-2: Design, synthesis and antimalarial efficacy studies.
Antimalarials
/ chemical synthesis
Cysteine Endopeptidases
/ metabolism
Dose-Response Relationship, Drug
Drug Design
Malaria, Falciparum
/ drug therapy
Molecular Structure
Parasitic Sensitivity Tests
Plasmodium falciparum
/ drug effects
Quinolines
/ chemical synthesis
Structure-Activity Relationship
Drug development
Falcipain-2 (FP2)
Malaria
P. falciparum
Quinoline carboxamide
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
03 2021
03 2021
Historique:
received:
21
07
2020
revised:
07
09
2020
accepted:
19
11
2020
pubmed:
8
12
2020
medline:
22
9
2021
entrez:
7
12
2020
Statut:
ppublish
Résumé
Targeting Falcipain-2 (FP2) for the development of antimalarials is a promising and established concept in antimalarial drug discovery and development. FP2, a member of papain-family cysteine protease of the malaria parasite Plasmodium falciparum holds an important role in hemoglobin degradation pathway. A new series of quinoline carboxamide-based compounds was designed, synthesized and evaluated for antimalarial activity. We integrated molecular hybridization strategy with in-silico drug design to develop FP2 inhibitors. In-vitro results of FP2 inhibition by Qs17, Qs18, Qs20 and Qs21 were found to be in low micromolar range with IC
Identifiants
pubmed: 33280833
pii: S0045-2068(20)31812-5
doi: 10.1016/j.bioorg.2020.104514
pii:
doi:
Substances chimiques
Antimalarials
0
Quinolines
0
quinoline
E66400VT9R
Cysteine Endopeptidases
EC 3.4.22.-
falcipain 2
EC 3.4.22.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
104514Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.