Identification of Isoflavone Derivatives as Effective Anticryptosporidial Agents in Vitro and in Vivo
| Autor: | Neil G. Berry, Shelley L. Moores, Eleanor C. Row, Andrew V. Stachulski, I.S. Adagu, A. C. Lilian Low, David C. Warhurst, Jean-Francois Rossignol |
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| Rok vydání: | 2006 |
| Předmět: |
Male
Antiparasitic medicine.drug_class Flavonoid Cryptosporidiosis Genistein Immunocompromised Host Structure-Activity Relationship chemistry.chemical_compound In vivo Cell Line Tumor Drug Discovery medicine Animals Humans Structure–activity relationship Cryptosporidium parvum chemistry.chemical_classification Isoflavones In vitro Biochemistry chemistry Cell culture Coccidiostats Molecular Medicine Cattle Female Gerbillinae |
| Zdroj: | Journal of Medicinal Chemistry. 49:1450-1454 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm050973f |
| Popis: | We report the preparation and antiparasitic activity in vitro and in vivo of a series of isoflavone derivatives related to genistein. These analogues retain the 5,7-dihydroxyisoflavone core of genistein: direct genistein analogues (2-H isoflavones), 2-carboethoxy isoflavones, and the precursor deoxybenzoins were all evaluated. Excellent in vitro activity against Cryptosporidium parvum was observed for both classes of isoflavones in cell cultures, and the lead compound 19, RM6427, shows high in vivo efficacy against an experimental infection. |
| Databáze: | OpenAIRE |
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