3535-27-1Relevant academic research and scientific papers
VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides
Reed, Carson W.,McGowan, Kevin M.,Spearing, Paul K.,Stansley, Branden J.,Roenfanz, Hanna F.,Engers, Darren W.,Rodriguez, Alice L.,Engelberg, Eileen M.,Luscombe, Vincent B.,Loch, Matthew T.,Remke, Daniel H.,Rook, Jerri M.,Blobaum, Anna L.,Conn, P. Jeffrey,Niswender, Colleen M.,Lindsley, Craig W.
supporting information, p. 1326 - 1330 (2017/12/26)
Herein, we report the structure-activity relationships within a series of mGlu7 NAMs based on an N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamide core with excellent CNS penetration (Kp 1.9-5.8 and Kp,uu 0.4-1.4). Analogues in this series displayed steep SAR. Of these, VU6010608 (11a) emerged with robust efficacy in blocking high frequency stimulated long-term potentiation in electrophysiology studies.
ANTIVIRAL COMPOUNDS
-
Paragraph 0705, (2015/03/13)
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
Inhibitors of Src tyrosine kinase: The preparation and structure-activity relationship of 4-anilino-3-cyanoquinolines and 4-anilinoquinazolines
Wang, Yanong D.,Miller, Karen,Boschelli, Diane H.,Ye, Fei,Wu, Biqi,Floyd,Powell, Dennis W.,Wissner, Allan,Weber, Jennifer M.,Boschelli, Frank
, p. 2477 - 2480 (2007/10/03)
Src is a nonreceptor tyrosine kinase involved in signaling pathways that control proliferation, migration, and angiogenesis. Increased Src expression and activity are associated with an increase in tumor malignancy and poor prognosis. Several quinolines and quinazolines were identified as potent and selective inhibitors of Src kinase activity. (C) 2000 Elsevier Science Ltd.
