Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents
| Autor: | Erika Smith, Chandrashekar Gudise, Yuling Zeng, Lai Wei, Shuren Zhu, Quan Zhang |
|---|---|
| Rok vydání: | 2009 |
| Předmět: |
Drug
media_common.quotation_subject Plasmodium falciparum Clinical Biochemistry Drug Evaluation Preclinical Pharmaceutical Science Pharmacology Biochemistry Article Antimalarials Mice Structure-Activity Relationship chemistry.chemical_compound Parasitic Sensitivity Tests Piperidines Drug Discovery Animals Antimalarial Agent Molecular Biology media_common Natural product Molecular Structure biology Chemistry Alkaloid Organic Chemistry Biological activity Dichroa febrifuga biology.organism_classification Acute toxicity Malaria Quinazolines Molecular Medicine Febrifugine Hydrangeaceae |
| Zdroj: | Bioorganic & Medicinal Chemistry. 17:4496-4502 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2009.05.011 |
| Popis: | Febrifugine is an alkaloid isolated from Dichroa febrifuga Lour as the active component against Plasmodium falciparum. Adverse side effects have precluded febrifugine as a potential clinical drug. In this study novel febrifugine analogues were designed and synthesized. Lower toxicity was achieved by reducing or eliminating the tendency of forming chemically reactive and toxic intermediates and metabolites. Synthesized compounds were evaluated for acute toxicity and in vitro and in vivo antimalarial efficacy. Some compounds are much less toxic than the natural product febrifugine and existing antimalarial drug chloroquine and are expected to possess wide therapeutic windows. These compounds, as well as the underlying design rationale, may find usefulness in the discovery and development of new antimalarial drugs. |
| Databáze: | OpenAIRE |
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