Aryl Bis-Sulfonamide Inhibitors of IspF from Arabidopsis thaliana and Plasmodium falciparum was written by Thelemann, Jonas;Illarionov, Boris;Barylyuk, Konstantin;Geist, Julie;Kirchmair, Johannes;Schneider, Petra;Anthore, Lucile;Root, Katharina;Trapp, Nils;Bacher, Adelbert;Witschel, Matthias;Zenobi, Renato;Fischer, Markus;Schneider, Gisbert;Diederich, Francois. And the article was included in ChemMedChem in 2015.Recommanded Product: 615-55-4 This article mentions the following:
2-Methylerythritol 2,4-cyclodiphosphate synthase (IspF) is an essential enzyme for the biosynthesis of isoprenoid precursors in plants and many human pathogens. The protein is an attractive target for the development of anti-infectives and herbicides. Using a photometric assay, a screen of 40,000 compounds on IspF from Arabidopsis thaliana afforded sym. aryl bis-sulfonamides that inhibit IspF from A. thaliana (AtIspF) and Plasmodium falciparum (PfIspF) with IC50 values in the micromolar range. The ortho-bis-sulfonamide structural motif is essential for inhibitory activity. The best derivatives obtained by parallel synthesis showed IC50 values of 1.4 μM against PfIspF and 240 nM against AtIspF. Substantial herbicidal activity was observed at a dose of 2 kg ha-1. Mol. modeling studies served as the basis for an in silico search targeted at the discovery of novel, non-sym. sulfonamide IspF inhibitors. The designed compounds were found to exhibit inhibitory activities in the double-digit micromolar IC50 range. In the experiment, the researchers used many compounds, for example, 3,4-Dibromoaniline (cas: 615-55-4Recommanded Product: 615-55-4).
3,4-Dibromoaniline (cas: 615-55-4) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Recommanded Product: 615-55-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary