5731-17-9Relevant articles and documents
Discovery of phenylpyrrolidine derivatives as a novel class of retinol binding protein 4 (RBP4) reducers
Nakamura, Shinji,Kamaura, Masahiro,Akao, Yuichiro,Nakamura, Natsuko,Mizukami, Atsushi,Goto, Akihiko,Furuyama, Naoki,Cho, Nobuo,Kasai, Shizuo
supporting information, (2021/12/30)
Retinol-binding protein 4 (RBP4) is a potential drug target for metabolic and ophthalmologic diseases. A high-throughput screening of our compound library has identified a small-molecule RBP4 reducer 7a, as a hit compound. Aiming to provide a suitable too
Design, synthesis, and characterization of novel, nonquaternary reactivators of GF-inhibited human acetylcholinesterase
McHardy, Stanton F.,Bohmann, Jonathan A.,Corbett, Michael R.,Campos, Bismarck,Tidwell, Michael W.,Thompson, Paul Marty,Bemben, Chris J.,Menchaca, Tony A.,Reeves, Tony E.,Cantrell Jr., William R.,Bauta, William E.,Lopez, Ambrosio,Maxwell, Donald M.,Brecht, Karen M.,Sweeney, Richard E.,McDonough, John
, p. 1711 - 1714 (2014/04/17)
The goal of this research was to identify structurally novel, non-quaternarypyridinium reactivators of GF (cyclosarin)-inhibited hAChE that possess the capacity to mediate in vitro reactivation of GF-inhibited human acetylcholinesterase (hAChE). New compounds were designed, synthesized and assessed in GF-inhibited hAChE assays. Structure activity relationships for AChE binding and reactivation of GF-inhibited hAChE were developed. Lead compounds from two different chemical series, represented by compounds 17 and 38, displayed proficient in vitro reactivation of GF-inhibited hAChE, while also possessing low inhibition of native enzyme.
Disubstituted pyrimidines as Lck inhibitors
Hunt, Julianne A.,Beresis, Richard T.,Goulet, Joung L.,Holmes, Mark A.,Hong, Xinfang J.,Kovacs, Ernest,Mills, Sander G.,Ruzek, Rowena D.,Wong, Frederick,Hermes, Jeffrey D.,Park, Young-Whan,Salowe, Scott P.,Sonatore, Lisa M.,Wu, Lin,Woods, Andrea,Zaller, Dennis M.,Sinclair, Peter J.
supporting information; experimental part, p. 5440 - 5443 (2010/04/26)
We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cell
