35216-03-6Relevant academic research and scientific papers
Development of new highly potent imidazo[1,2-b[pyridazines targeting Toxoplasma gondii calcium-dependent protein kinase 1
Moine, Espérance,Dimier-Poisson, Isabelle,Enguehard-Gueiffier, Cécile,Logé, Cédric,Pénichon, Mélanie,Moiré, Nathalie,Delehouzé, Claire,Foll-Josselin, Beátrice,Ruchaud, Sandrine,Bach, Stéphane,Gueiffier, Alain,Debierre-Grockiego, Fran?oise,Denevault-Sabourin, Caroline
, p. 80 - 105 (2015/11/02)
Using a structure-based design approach, we have developed a new series of imidazo[1,2-b]pyridazines, targeting the calcium-dependent protein kinase-1 (CDPK1) from Toxoplasma gondii. Twenty derivatives were thus synthesized. Structure-activity relationships and docking studies confirmed the binding mode of these inhibitors within the ATP binding pocket of TgCDPK1. Two lead compounds (16a and 16f) were then identified, which were able to block TgCDPK1 enzymatic activity at low nanomolar concentrations, with a good selectivity profile against a panel of mammalian kinases. The potential of these inhibitors was confirmed in vitro on T. gondii growth, with EC50 values of 100 nM and 70 nM, respectively. These best candidates also displayed low toxicity to mammalian cells and were selected for further in vivo investigations on murine model of acute toxoplasmosis.
AgONO-Assisted Direct C-H Arylation of Heteroarenes with Anilines
Gowrisankar, Saravanan,Seayad, Jayasree
supporting information, p. 12754 - 12758 (2015/03/30)
A novel copper-catalyzed C-H arylation of heteroarenes with anilines by an in situ diazonium reaction is established by using silver nitrite (AgONO) as an unconventional nitrosating reagent under acid-free conditions. It provides a complementary approach for the C-H arylation of electron-rich heteroarenes with aromatic amines affording a variety of heterobiaryls in moderate to good yields.
Direct 2-arylation of thiophene using low loading of a phosphine-free palladium catalyst
Bensaid, Souhila,Roger, Julien,Beydoun, Kassem,Roy, David,Doucet, Henri
experimental part, p. 3524 - 3531 (2011/09/16)
The direct coupling of aryl halides with thiophene would be a considerable advantage for sustainable development because of only HBr associated with a base as by-product is formed and the number of steps to prepare these compounds is less than in more cla
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase
Gattinoni, Sonia,Simone, Chiara De,Dallavalle, Sabrina,Fezza, Filomena,Nannei, Raffaella,Battista, Natalia,Minetti, Patrizia,Quattrociocchi, Gianandrea,Caprioli, Antonio,Borsini, Franco,Cabri, Walter,Penco, Sergio,Merlini, Lucio,MacCarrone, Mauro
supporting information; experimental part, p. 4406 - 4411 (2010/10/02)
A series of oxime carbamates have been identified as potent inhibitors of fatty acid amide hydrolase (FAAH), an important regulatory enzyme of the endocannabinoid signaling system. Kinetic analysis indicates that they behave as non-competitive, reversible
