Identification of Isoflavone Derivatives as Effective Anticryptosporidial Agents in Vitro and in Vivo
Andrew V. StachulskiRomark Centre for Drug Discovery, Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K., Romark Research Laboratory, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, U.K., and Romark Institute for Medical Research, 6200 Courtney Campbell Causeway, Suite 200, Tampa, Florida 33607Neil G. BerryRomark Centre for Drug Discovery, Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K., Romark Research Laboratory, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, U.K., and Romark Institute for Medical Research, 6200 Courtney Campbell Causeway, Suite 200, Tampa, Florida 33607Audrey LowLondon School of Hygiene & Tropical MedicineShelley L. MooresRomark Centre for Drug Discovery, Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K., Romark Research Laboratory, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, U.K., and Romark Institute for Medical Research, 6200 Courtney Campbell Causeway, Suite 200, Tampa, Florida 33607Eleanor C. RowRomark Centre for Drug Discovery, Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K., Romark Research Laboratory, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, U.K., and Romark Institute for Medical Research, 6200 Courtney Campbell Causeway, Suite 200, Tampa, Florida 33607David C. WarhurstRomark Centre for Drug Discovery, Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K., Romark Research Laboratory, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, U.K., and Romark Institute for Medical Research, 6200 Courtney Campbell Causeway, Suite 200, Tampa, Florida 33607I. S. AdaguRomark Centre for Drug Discovery, Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K., Romark Research Laboratory, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, U.K., and Romark Institute for Medical Research, 6200 Courtney Campbell Causeway, Suite 200, Tampa, Florida 33607Jean‐François RossignolRomark Centre for Drug Discovery, Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K., Romark Research Laboratory, London School of Hygiene and Tropical Medicine, London, WC1E 7HT, U.K., and Romark Institute for Medical Research, 6200 Courtney Campbell Causeway, Suite 200, Tampa, Florida 33607
2006en
ABI
Аннотация
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.
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