243869-56-9Relevant articles and documents
Liver X receptor agonists with selectivity for LXRβ; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides
Swahn, Britt-Marie,Macsari, Istvan,Viklund, Jenny,Oehberg, Liselotte,Sjoedin, Johanna,Neelissen, Jan,Lindquist, Johanna
scheme or table, p. 2009 - 2012 (2009/11/30)
The synthesis and SAR of a new series of LXR agonist is reported. The N-Aryl-3,3,3-trifluoro-2-hydroxy-2-methyl-propionamide hits were found in a limited screen of the AstraZeneca compound collection. The effort to optimize these hits into LXRβ selectivity is described. Compound 20 displayed desirable pharmacokinetic profile and up regulation of ABCA1 and ABCG1 mRNA in the brain were achieved when evaluated in vivo in mice.
Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase
Bebernitz, Gregory R.,Aicher, Thomas D.,Stanton, James L.,Gao, Jiaping,Shetty, Suraj S.,Knorr, Douglas C.,Strohschein, Robert J.,Tan, Jennifer,Brand, Leonard J.,Liu, Charles,Wang, Wei H.,Vinluan, Christine C.,Kaplan, Emma L.,Dragland, Carol J.,DelGrande, Dominick,Islam, Amin,Lozito, Robert J.,Liu, Xilin,Maniara, Wieslawa M.,Mann, William R.
, p. 2248 - 2257 (2007/10/03)
The optimization of a series of anilide derivatives of (R)-3,3,3- trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase (PDHK) is described that started from N-phenyl-3,3,3- trifluoro-2-hydroxy-2-methylpropanamide 1 (IC
N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropanamides: K(ATP) potassium channel openers. Modifications on the western region
Ohnmacht, Cyrus J.,Russell, Keith,Empfield, James R.,Frank, Cathy A.,Gibson, Keith H.,Mayhugh, Daniel R.,McLaren, Frances M.,Shapiro, Howard S.,Brown, Frederick J.,Trainor, Diane A.,Ceccarelli, Christopher,Lin, Margaret M.,Masek, Brian B.,Forst, Janet M.,Harris, Robert J.,Hulsizer, James M.,Lewis, Joseph J.,Silverman, Stuart M.,Smith, Reed W.,Warwick, Paul J.,Kau, Sen T.,Chun, Alexa L.,Grant, Thomas L.,Howe, Burton B.,Li, Jack H.,Trivedi, Shephali,Halterman, Tracy J.,Yochim, Christopher,Dyroff, Martin C.,Kirkland,Neilson, Kathleen L.
, p. 4592 - 4601 (2007/10/03)
A subset of antiandrogen compounds, the N-aryl-3,3,3-trifluoro-2- hydroxy-2-methylpropanamides 1, were found to activate ATP sensitive potassium channels (K(ATP)) and represent a new class of potassium channel openers (PCOs). A structure-activity relation
