910249-35-3Relevant academic research and scientific papers
INHIBITORS OF FATTY ACID SYNTHASE (FAS)
-
Page/Page column 34; 38, (2008/06/13)
The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors
Rivkin, Alexey,Kim, Yoona R.,Goulet, Mark T.,Bays, Nathan,Hill, Armetta D.,Kariv, Ilona,Krauss, Stefan,Ginanni, Nicole,Strack, Peter R.,Kohl, Nancy E.,Chung, Christine C.,Varnerin, Jeffrey P.,Goudreau, Paul N.,Chang, Amy,Tota, Michael R.,Munoz, Benito
, p. 4620 - 4623 (2007/10/03)
A series of 3-aryl-4-hydroxyquinolin-2(1H)-ones with fatty acid synthase inhibitory activity was prepared. Starting from a derivative with an IC50 = 1.4 μM, SAR studies led to compounds with more than 70-fold increase in potency (IC50/sub
Quinolones as gonadotropin releasing hormone (GnRH) antagonists: Simultaneous optimization of the C(3)-aryl and C(6)-substituents
Young, Jonathan R.,Huang, Song X.,Chen, Irene,Walsh, Thomas F.,DeVita, Robert J.,Wyvratt Jr., Matthew J.,Goulet, Mark T.,Ren, Ning,Lo, Jane,Yang, Yi Tien,Yudkovitz, Joel B.,Cheng, Kang,Smith, Roy G.
, p. 1723 - 1727 (2007/10/03)
A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of substitution patterns of the 3-aryl substituent are described. The 3,4,5-trimethylphenyl substituent (23h) was found to be optimal. (C) 2000 Elsevier Science Ltd. All rights reserved.
