243869-56-9Relevant academic research and scientific papers
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.
Benzenesulfonamide-derivatives and their use as medicaments
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Page column 77, (2010/11/30)
Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N
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
4-Sulfonamidoanilide tertiary carbinols: A novel series of potassium channel openers
Empfield,Mayhugh,Ohnmacht,Frank,Grant,Li
, p. 775 - 778 (2007/10/03)
Sulfonamides are viable replacements for the phenylsulfonyl and benzoyl moieties initially described for the anilide tertiary carbinol series of K(ATP) potassium channel openers. The SAR of this new series and the synthetic chemistry employed to generate its members are described.
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
