2. Academic Validation
  3. Identification of isoflavone derivatives as effective anticryptosporidial agents in vitro and in vivo

Identification of isoflavone derivatives as effective anticryptosporidial agents in vitro and in vivo

  • J Med Chem. 2006 Feb 23;49(4):1450-4. doi: 10.1021/jm050973f.
Andrew V Stachulski 1,  Neil G Berry,  A C Lilian Low,  Shelley L Moores,  Eleanor Row,  David C Warhurst,  Ipemida S Adagu,  Jean-François Rossignol
Affiliations

Affiliation

  • 1 Romark Centre for Drug Discovery, Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, UK. [email protected]
PMID: 16480281 DOI: 10.1021/jm050973f
Abstract

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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