351439-07-1Relevant articles and documents
Palladium-catalysed functionalisation at 4- and 6- position of the 7-azaindole system
Allegretti, Marcello,Arcadi, Antonio,Marinelli, Fabio,Nicolini, Luca
, p. 609 - 612 (2001)
The synthesis of 4- and 6-substituted-7 azaindales through palladium-catalysed coupling reactions of the corresponding halosubstituted-7-azaindoles is described.
Selective inhibition of Helicobacter pylori methionine aminopeptidase by azaindole hydroxamic acid derivatives: Design, synthesis, in vitro biochemical and structural studies
Bala, Sandeepchowdary,Yellamanda, Kalisha vali,Kadari, Anilkumar,Ravinuthala, Venkata.S.U.,Kattula, Bhavita,Singh, Om V.,Gundla, Rambabu,Addlagatta, Anthony
, (2021/08/03)
Methionine aminopeptidases (MetAPs) are an important class of enzymes that work co-translationally for the removal of initiator methionine. Chemical inhibition or gene knockdown is lethal to the microbes suggesting that they can be used as antibiotic targ
Design of small molecule inhibitors of acetyl-CoA carboxylase 1 and 2 showing reduction of hepatic malonyl-CoA levels in vivo in obese Zucker rats
Bengtsson, Christoffer,Blaho, Stefan,Saitton, David Blomberg,Brickmann, Kay,Broddefalk, Johan,Davidsson, ?jvind,Drmota, Tomas,Folmer, Rutger,Hallberg, Kenth,Hallén, Stefan,Hovland, Ragnar,Isin, Emre,Johannesson, Petra,Kull, Bengt,Larsson, Lars-Olof,L?fgren, Lars,Nilsson, Kristina E.,Noeske, Tobias,Oakes, Nick,Plowright, Alleyn T.,Schnecke, Volker,Sthlberg, Pernilla,S?rme, Pernilla,Wan, Hong,Wellner, Eric,?ster, Linda
supporting information; experimental part, p. 3039 - 3053 (2011/06/27)
Inhibition of acetyl-CoA carboxylases has the potential for modulating long chain fatty acid biosynthesis and mitochondrial fatty acid oxidation. Hybridization of weak inhibitors of ACC2 provided a novel, moderately potent but lipophilic series. Optimization led to compounds 33 and 37, which exhibit potent inhibition of human ACC2, 10-fold selectivity over inhibition of human ACC1, good physical and in vitro ADME properties and good bioavailability. X-ray crystallography has shown this series binding in the CT-domain of ACC2 and revealed two key hydrogen bonding interactions. Both 33 and 37 lower levels of hepatic malonyl-CoA in vivo in obese Zucker rats.