215809-15-7Relevant academic research and scientific papers
Novel phenyl(thio)ureas bearing (thio)oxothiazoline group as potential BACE-1 inhibitors: Synthesis and biological evaluation
Andreoli, Federico,Doukara, Abdallah Larbi,Mehdid, Mohammed Amine,Vanthuyne, Nicolas,Roussel, Christian,Dessolin, Jean,Kraus, Jean-Louis
, p. 153 - 162 (2013/04/23)
We report the synthesis and the β-site amyloid precursor protein cleaving enzyme-1 inhibitory properties of novel phenyl(thio)ureas bearing 2-(thio)oxothiazoline derivatives. A library of analogues was prepared according to specific synthetic schemes and the inhibitory activity was monitored using a fluorescence resonance energy transfer assay. Several analogues show potent inhibitory activities ranging between 1 and 0.01 μM and the activity is related to the NH acidity of the (thio)urea motif. Our results illustrate once again the close relationship between molecular recognition, complexation of the active site in enzymatic system, and organocatalysis utilizing explicit hydrogen bonding.
Towards functionalised quasi-planar dithiadiazafulvalenes: Synthesis of various precursors
Bellec, Nathalie,Lorcy, Dominique,Robert, Albert
, p. 1442 - 1446 (2007/10/03)
The synthesis of 1,2-bis(2-thioxo-2,3-dihydrothiazol-3-yl)benzenes and 1,2-bis(2-selenoxo-2,3-dihydrothiazol-3-yl)benzenes precursors of quasi- planar dithiadiazafulvalenes, is described. Functionalisation of these derivatives via lithiation is also reported.
