Aminopropyl-Linked Quinoline-Triazole Hybrids with Enhanced Antiplasmodial Activity Targeting β-Hematin Formation

Resistance of Plasmodium falciparum to current antimalarials necessitates new therapies. This preliminary study presents the design, synthesis, and characterization of novel 7-chloroquinoline-1,2,3-triazole hybrids incorporating aminopropyl linkers. Several compounds show submicromolar in vitro activity against both chloroquine-sensitive and -resistant strains. β-Hematin inhibition assays revealed strong activity, especially for a cationic iridium(III) complex (7), despite its limited cellular efficacy. The presence of an aminoalkyl linker, secondary amines, and metal coordination were found to be critical to enhanced antiplasmodial activity, supporting further development of these hybrids as promising antimalarial agents.

Authors

Institutions

Publication Details

Journal
Organometallics
Published
2025-10-13
DOI
https://doi.org/10.1021/acs.organomet.5c00294
Primary Topic
Click Chemistry and Applications
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Aminopropyl-Linked Quinoline-Triazole Hybrids with Enhanced Antiplasmodial Activity Targeting β-Hematin Formation

Gregory S. Smith, Diana R. Melis
Organometallics
Click Chemistry and Applications
article

Aminopropyl-Linked Quinoline-Triazole Hybrids with Enhanced Antiplasmodial Activity Targeting β-Hematin Formation

Gregory S. Smith, Diana R. Melis
article en

Abstract

Resistance of Plasmodium falciparum to current antimalarials necessitates new therapies. This preliminary study presents the design, synthesis, and characterization of novel 7-chloroquinoline-1,2,3-triazole hybrids incorporating aminopropyl linkers. Several compounds show submicromolar in vitro activity against both chloroquine-sensitive and -resistant strains. β-Hematin inhibition assays revealed strong activity, especially for a cationic iridium(III) complex (7), despite its limited cellular efficacy. The presence of an aminoalkyl linker, secondary amines, and metal coordination were found to be critical to enhanced antiplasmodial activity, supporting further development of these hybrids as promising antimalarial agents.

OrganometallicsVol. 44(20)
University of Cape Town (ZA)
Openalex Percentile: Top 78%
Click Chemistry and Applications
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.