26672-58-2Relevant articles and documents
Cobalt-Catalyzed Migrational Isomerization of Styrenes
Zhao, Jiajin,Cheng, Biao,Chen, Chenhui,Lu, Zhan
supporting information, p. 837 - 841 (2020/01/31)
An efficient cobalt-catalyzed migrational isomerization of styrenes was developed using the thiazoline iminopyridine (TIP) ligand. This reaction is operationally simple and atom-economical using readily available starting materials to access trisubstituted alkenes. Even when using a 0.1 mol % catalyst loading, the reaction could be conducted in neat and completed in 1 h with excellent conversion and high E stereoselectivity.
Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis
Hong, W. David,Gibbons, Peter D.,Leung, Suet C.,Amewu, Richard,Stocks, Paul A.,Stachulski, Andrew,Horta, Pedro,Cristiano, Maria L. S.,Shone, Alison E.,Moss, Darren,Ardrey, Alison,Sharma, Raman,Warman, Ashley J.,Bedingfield, Paul T. P.,Fisher, Nicholas E.,Aljayyoussi, Ghaith,Mead, Sally,Caws, Maxine,Berry, Neil G.,Ward, Stephen A.,Biagini, Giancarlo A.,O’Neill, Paul M.,Nixon, Gemma L.
supporting information, p. 3703 - 3726 (2017/05/19)
A high-throughput screen (HTS) was undertaken against the respiratory chain dehydrogenase component, NADH:menaquinone oxidoreductase (Ndh) of Mycobacterium tuberculosis (Mtb). The 11000 compounds were selected for the HTS based on the known phenothiazine Ndh inhibitors, trifluoperazine and thioridazine. Combined HTS (11000 compounds) and in-house screening of a limited number of quinolones (50 compounds) identified ～100 hits and four distinct chemotypes, the most promising of which contained the quinolone core. Subsequent Mtb screening of the complete in-house quinolone library (350 compounds) identified a further ～90 hits across three quinolone subtemplates. Quinolones containing the amine-based side chain were selected as the pharmacophore for further modification, resulting in metabolically stable quinolones effective against multi drug resistant (MDR) Mtb. The lead compound, 42a (MTC420), displays acceptable antituberculosis activity (Mtb IC50 = 525 nM, Mtb Wayne IC50 = 76 nM, and MDR Mtb patient isolates IC50 = 140 nM) and favorable pharmacokinetic and toxicological profiles.
Tethered η5-oxocyclohexadienyl piano-stool ruthenium(II) complexes: A new class of catalysts?
Kechaou-Perrot, Manel,Vendier, Laure,Bastin, Stphanie,Sotiropoulos, Jean-Marc,Miqueu, Karinne,Menndez-Rodrguez, Luca,Crochet, Pascale,Cadierno, Victorio,Igau, Alain
supporting information, p. 6294 - 6297 (2015/02/19)
The straightforward synthesis of tethered η5-oxocyclohexadienyl Ru(II) complexes is presented. Pioneering results in catalysis show that these original half-sandwich Ru(II) complexes allow the effective isomerization of allylic alcohols under mild conditions without further additives; η5-oxocyclohexadienyl ruthenium complexes may be considered as a new class of catalysts.
