Back to Search
Start Over
New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities
- Source :
- Molecules; Volume 18; Issue 4; Pages: 4718-4727, Dadun. Depósito Académico Digital de la Universidad de Navarra, instname, Molecules, Repositorio UdeA, Universidad de Antioquia, instacron:Universidad de Antioquia, Molecules, 2013, 18 (4), pp.4718-4727. ⟨10.3390/molecules18044718⟩, Molecules, Vol 18, Iss 4, Pp 4718-4727 (2013)
- Publication Year :
- 2013
- Publisher :
- MDPI, 2013.
-
Abstract
- International audience; Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Continuing with our efforts to identify new compounds active against malaria and leishmaniasis, twelve new 1,4-di-N-oxide quinoxaline derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum FCR-3 strain, Leishmania infantum and Leishmania amazonensis. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. The results obtained indicate that a cyclopentyl derivative had the best antiplasmodial activity (2.9 µM), while a cyclohexyl derivative (2.5 µM) showed the best activity against L. amazonensis, and a 3-chloropropyl derivative (0.7 µM) showed the best results against L. infantum. All these compounds also have a Cl substituent in the R7 position
- Subjects :
- Plasmodium
[SDV]Life Sciences [q-bio]
Pharmaceutical Science
leishmanicidal
Antiplasmodial
4-di-N-Oxide
Analytical Chemistry
chemistry.chemical_compound
Parasitic Sensitivity Tests
Amide
Chlorocebus aethiops
Drug Discovery
Leishmania infantum
Leishmania
Antiparasitic Agents
biology
Oxides
Chemistry (miscellaneous)
Molecular Medicine
Quinoxaline
Stereochemistry
Plasmodium falciparum
Substituent
Article
lcsh:QD241-441
quinoxaline
1,4-di-N-oxide
antiplasmodial
Antimalarials
Inhibitory Concentration 50
Structure-Activity Relationship
lcsh:Organic chemistry
Quinoxalines
parasitic diseases
medicine
Animals
Humans
Physical and Theoretical Chemistry
Vero Cells
Leishmanicidal
Organic Chemistry
Leishmaniasis
biology.organism_classification
medicine.disease
Amides
In vitro
chemistry
Vero cell
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Database :
- OpenAIRE
- Journal :
- Molecules; Volume 18; Issue 4; Pages: 4718-4727, Dadun. Depósito Académico Digital de la Universidad de Navarra, instname, Molecules, Repositorio UdeA, Universidad de Antioquia, instacron:Universidad de Antioquia, Molecules, 2013, 18 (4), pp.4718-4727. ⟨10.3390/molecules18044718⟩, Molecules, Vol 18, Iss 4, Pp 4718-4727 (2013)
- Accession number :
- edsair.doi.dedup.....02ced1f632da8f03cd8c80f2c57ad9ff
- Full Text :
- https://doi.org/10.3390/molecules18044718⟩