4-Anilinoquinoline triazines: A novel class of hybrid antimalarial agents
| Autor: | Jitendra K. Sexana, S. Raja Kumar, Mohammad Imran Siddiqi, Kumkum Srivastava, Ashok Kumar, Prem M. S. Chauhan, Sunil Kumar Puri |
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| Rok vydání: | 2011 |
| Předmět: |
Hemeproteins
Models Molecular Stereochemistry Plasmodium falciparum Stereoisomerism Antimalarials Mice Structure-Activity Relationship chemistry.chemical_compound Parasitic Sensitivity Tests Chlorocebus aethiops Drug Discovery medicine Animals Structure–activity relationship Moiety Antimalarial Agent Cytotoxicity Vero Cells Cell Proliferation Triazine Pharmacology Molecular Structure Triazines Chemistry Organic Chemistry General Medicine In vitro Malaria Mechanism of action Quinolines medicine.symptom |
| Zdroj: | European Journal of Medicinal Chemistry. 46:676-690 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2010.12.003 |
| Popis: | A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum as well as for their cytotoxicity toward VERO cell line. Five compounds (19, 20, 23, 41 and 45) exhibited the antimalarial potency superior to CQ. Compounds 14 and 16 were found to be orally active at a dose of 100 mg/kg×4 days against CQ-resistant strain of P. yoelii. Inhibition of β-hematin formation assay and molecular docking study has been conducted in order to gain insight into the mechanism of action of proposed targets for the 4-anilinoquinoline and triazine moiety of the hybrid compounds. |
| Databáze: | OpenAIRE |
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