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Piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates: Synthesis and antiplasmodial evaluation
- Source :
- Chemical biologydrug design. 90(4)
- Publication Year :
- 2017
-
Abstract
- A series of piperazine-linked 4-aminoquinoline-chalcone/ferrocenyl-chalcone conjugates were prepared with a view to evaluate their activities against Plasmodium falciparum. The synthesized conjugates had in vitro IC50 values from 0.41 to 2.38 μm against chloroquine-resistant and mefloquine-sensitive W2 strain of P. falciparum. The submicromolar activities of most of the synthesized conjugates suggest that such molecular frameworks can act as therapeutic templates for the design and synthesis of new antimalarials.
- Subjects :
- 0301 basic medicine
Chalcone
Plasmodium falciparum
Drug Resistance
01 natural sciences
Biochemistry
Piperazines
03 medical and health sciences
chemistry.chemical_compound
Antimalarials
parasitic diseases
Drug Discovery
Structure–activity relationship
Humans
Ferrous Compounds
Aminoquinolines
Malaria, Falciparum
Pharmacology
biology
010405 organic chemistry
Organic Chemistry
Chloroquine
biology.organism_classification
Combinatorial chemistry
0104 chemical sciences
Piperazine
030104 developmental biology
chemistry
4-Aminoquinoline
Molecular Medicine
Aldol condensation
Conjugate
HeLa Cells
Subjects
Details
- ISSN :
- 17470285
- Volume :
- 90
- Issue :
- 4
- Database :
- OpenAIRE
- Journal :
- Chemical biologydrug design
- Accession number :
- edsair.doi.dedup.....f04bb259c3c1d4e0e70b87c7e2981026