Format

Send to

Choose Destination
See comment in PubMed Commons below
Eur J Med Chem. 2013 Jul;65:376-80. doi: 10.1016/j.ejmech.2013.04.030. Epub 2013 Apr 23.

Evaluation of Jatropha isabelli natural products and their synthetic analogs as potential antimalarial therapeutic agents.

Author information

  • 1Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105-3678, USA.

Abstract

Protozoal diseases such as malaria are a leading world health concern. We screened a library of fractionated natural products to identify new potential therapeutic leads and discovered that jatrophone (a product of Jatropha isabelli) exerts significant activity against Plasmodium falciparum strains 3D7 and K1. A focused jatrophone-scaffold library was synthesized to evaluate jatrophone's mode of action and identify more selective analogs. Compounds 25 and 32 of this natural product-inspired compound library exhibited micromolar EC50 values against strains 3D7 and K1, thus providing a new antimalarial molecular scaffold. Our report describes an efficient derivatization approach used to evaluate the structure-activity relationship of jatrophone analogs in search of potential new antimalarial agents.

Published by Elsevier Masson SAS.

KEYWORDS:

1-butyl-3-methylimidazolium tetrafluoroborate; Antimalarial agents; Conjugated additions; Jatropha isabelli; Jatrophone; N-bromosuccinimide; NBS; PAMPA; Plasmodium falciparum; [bmim][BF(4)]; mCPBA; meta-chloroperoxybenzoic acid; parallel artificial membrane permeability assay

[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Write to the Help Desk