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Discovery of highly selective 7-chloroquinoline-thiohydantoins with potent antimalarial activity
- Source :
- European Journal of Medicinal Chemistry. 84:425-432
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- A series of C-3 thiourea functionalized β -lactams, β -lactam-7-chloroquinoline conjugates and 7-chloroquinoline-thiohydantoin derivatives were prepared with the aim of probing antimalarial structure–activity relationships. 7-Chlorquinoline-thiohydantoin derivatives were found to be potent inhibitors of cultured Plasmodium falciparum , with the most potent and non-cytotoxic compound exhibiting an IC 50 of 39.8 nM. Studies of β -hematin formation suggested that inhibition of haemozoin formation could be primary mechanism of action, with IC 50 values comparable to those of chloroquine. Evaluation of cytotoxicity against HeLa cells demonstrated high selective indices.
- Subjects :
- Stereochemistry
Plasmodium falciparum
HeLa
Antimalarials
Structure-Activity Relationship
chemistry.chemical_compound
Parasitic Sensitivity Tests
Chloroquine
Drug Discovery
medicine
Humans
Cytotoxicity
Cell Proliferation
Pharmacology
Dose-Response Relationship, Drug
Molecular Structure
biology
Organic Chemistry
General Medicine
biology.organism_classification
Highly selective
Combinatorial chemistry
Thiohydantoins
Mechanism of action
Thiourea
chemistry
Aminoquinolines
medicine.symptom
HeLa Cells
Conjugate
medicine.drug
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 84
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....feaea7beccd5f51ad5b1a7801c39d7e0