Solution-phase parallel synthesis of substituted chalcones and their antiparasitary activity against Giardia lamblia
| Autor: | Francisco Delgado-Vargas, Julio Montes-Avila, Ignacio A. Rivero, Josefina Sicairos-Félix, Sylvia Páz Díaz-Camacho |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
Antiparasitic
medicine.drug_class Clinical Biochemistry Flavonoid Antiprotozoal Agents Pharmaceutical Science Microbial Sensitivity Tests medicine.disease_cause Biochemistry Medicinal chemistry Chemical synthesis Inhibitory Concentration 50 Structure-Activity Relationship Chalcones Drug Discovery medicine Structure–activity relationship Giardia lamblia Organic chemistry Animals Molecular Biology chemistry.chemical_classification Chemistry Organic Chemistry Biological activity Solution phase Molecular Medicine Aldol condensation |
| Zdroj: | Bioorganicmedicinal chemistry. 17(18) |
| ISSN: | 1464-3391 |
| Popis: | A library of 25-membered chalcones was prepared by parallel synthesis. Substituted acetophenones and benzaldehydes were condensed using the Claisen-Schmidt base-catalyzed aldol condensation. Several chalcones showed in vitro antiparasitic activity against Giardia lamblia. The highest activity observed for the IC(50) values were 12.72, 15.05 and 15.31 microg/mL, respectively; these are potential leads for the development of antigiardial compounds. |
| Databáze: | OpenAIRE |
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