| Literature DB >> 23747806 |
Victor Hadi1, Megan Hotard, Taotao Ling, Yandira G Salinas, Gustavo Palacios, Michele Connelly, Fatima Rivas.
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.Entities:
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
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Year: 2013 PMID： 23747806 DOI： 10.1016/j.ejmech.2013.04.030
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514