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Synthesis and biological evaluation of 2,3-diarylimidazo[1,2-a]pyridines as antileishmanial agents
- Source :
- European Journal of Medicinal Chemistry, European Journal of Medicinal Chemistry, 2012, 58, pp.543-556. ⟨10.1016/j.ejmech.2012.10.048⟩
- Publication Year :
- 2012
-
Abstract
- International audience; A novel series of 2,3-diarylimidazo[1,2-a]pyridines was synthesized and evaluated for their antileishmanial activities. Four derivatives exhibited good activity against the promastigote and intracellular amastigote stages of Leishmania major, coupled with a low cytotoxicity against the HeLa human cell line. The impact of compound lipophilicity on antiparasitic activities was investigated by Log D comparison. Although LmCK1 could be the parasitic target for three compounds (13, 18, 21), the inhibition of another target is under study to explain the antileishmanial effect of the most promising compounds.
- Subjects :
- Models, Molecular
Antiparasitic
medicine.drug_class
Pyridines
[SDV]Life Sciences [q-bio]
Casein kinase 1
Antiprotozoal Agents
Antineoplastic Agents
Direct arylation
HeLa
Structure-Activity Relationship
Parasitic Sensitivity Tests
Lipophilicity
Drug Discovery
medicine
[CHIM]Chemical Sciences
Humans
Leishmania major
Amastigote
Cytotoxicity
Protein Kinase Inhibitors
Protein Kinase C
Antileishmanial activity 2
Biological evaluation
Cell Proliferation
Pharmacology
biology
Dose-Response Relationship, Drug
Molecular Structure
Chemistry
Casein Kinase I
Organic Chemistry
General Medicine
Antileishmanial activity
biology.organism_classification
Combinatorial chemistry
Antileishmanial activity 2 3-Diarylimidazo[1 2-a]pyridines Direct arylation Lipophilicity Casein kinase 1
3-Diarylimidazo[1
[SDV.TOX]Life Sciences [q-bio]/Toxicology
2-a]pyridines Direct arylation Lipophilicity Casein kinase 1
[SDV.SP.PHARMA]Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology
Drug Screening Assays, Antitumor
2-a]pyridines
Intracellular
HeLa Cells
Subjects
Details
- ISSN :
- 17683254 and 02235234
- Volume :
- 58
- Database :
- OpenAIRE
- Journal :
- European journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....544d2ee66881a344587c8c70e60eca4e
- Full Text :
- https://doi.org/10.1016/j.ejmech.2012.10.048⟩