1196156-42-9Relevant articles and documents
Zinc Acetate-Promoted Buchwald-Hartwig Couplings of Heteroaromatic Amines
Ayothiraman, Rajaram,Rangaswamy, Sundaramurthy,Maity, Prantik,Simmons, Eric M.,Beutner, Gregory L.,Janey, Jacob,Treitler, Daniel S.,Eastgate, Martin D.,Vaidyanathan, Rajappa
supporting information, p. 7420 - 7427 (2017/07/26)
Zinc salts have been shown to promote the Buchwald-Hartwig coupling of azaindoles and azaindazoles with heteroaryl chlorides to provide the corresponding 1-aryl-1H-azaindoles and 1-aryl-1H-azaindazoles. The substrate scope and mechanistic aspects of this reaction were explored.
Reversible Inhibitors Arrest ClpP in a Defined Conformational State that Can Be Revoked by ClpX Association
Pahl, Axel,Lakemeyer, Markus,Vielberg, Marie-Theres,Hackl, Mathias W.,Vomacka, Jan,Korotkov, Vadim S.,Stein, Martin L.,Fetzer, Christian,Lorenz-Baath, Katrin,Richter, Klaus,Waldmann, Herbert,Groll, Michael,Sieber, Stephan A.
supporting information, p. 15892 - 15896 (2016/01/29)
Caseinolytic protease P (ClpP) is an important regulator of Staphylococcus aureus pathogenesis. A high-throughput screening for inhibitors of ClpP peptidase activity led to the identification of the first non-covalent binder for this enzyme class. Co-crystallization of the small molecule with S. aureus ClpP revealed a novel binding mode: Because of the rotation of the conserved residue proline 125, ClpP is locked in a defined conformational state, which results in distortion of the catalytic triad and inhibition of the peptidase activity. Based on these structural insights, the molecule was optimized by rational design and virtual screening, resulting in derivatives exceeding the potency of previous ClpP inhibitors. Strikingly, the conformational lock is overturned by binding of ClpX, an associated chaperone that enables proteolysis by substrate unfolding in the ClpXP complex. Thus, regulation of inhibitor binding by associated chaperones is an unexpected mechanism important for ClpP drug development.
GPR40 RECEPTOR AGONIST, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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Paragraph 1389-1393;1501-1503, (2014/05/24)
The present invention relates to a novel compound having GPR40 receptor agonist activity that promotes insulin secretion and inhibits blood sugar rise after glucose loading, and is thereby useful for the treatment of diabetes and complications thereof, the preparation method thereof and pharmaceutical composition containing them as an active ingredient.