ChemMedChem

Cover image for Vol. 12 Issue 10

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

May 22, 2010

VIP: Thiazolopyrimidine Inhibitors of 2-Methylerythritol 2,4-Cyclodiphosphate Synthase (IspF) from Mycobacterium tuberculosis and Plasmodium falciparum

VIP: Thiazolopyrimidine Inhibitors of 2-Methylerythritol 2,4-Cyclodiphosphate Synthase (IspF) from Mycobacterium tuberculosis and Plasmodium falciparumJulie G. Geist, Susan Lauw, Victoria Illarionova, Boris Illarionov, Markus Fischer,* Tobias Gräwert, Felix Rohdich, Wolfgang Eisenreich, Johannes Kaiser, Michael Groll,* Christian Scheurer, Sergio Wittlin, Jose L. Alonso-Gomez, W. Bernd Schweizer, Adelbert Bacher, and Francois Diederich*

Pathogenic organisms biosynthesize isoprenoids via the non-mevalonate pathway, whereas mammals obtain isoprenoids by the mevalonate route. Therefore, compounds that inhibit enzymes of the former pathway are expected to lack target-related toxicity. Diederich and colleagues identified heterocyclic inhibitors of a key non-mevalonate pathway enzyme, IspF, in their screen of a random compound library. Several of the compounds identified have IC50 values in the low single-digit micromolar range, despite the library's relatively small size.

Received February 25, 2010; published online May 17, 2010, DOI: 10.1002/cmdc.201000083.

Your Comment...

[Browse more news]

SEARCH

SEARCH BY CITATION