220746-98-5Relevant academic research and scientific papers
Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression
Pirat, Celine,Dacquet, Catherine,Leclerc, Veronique,Hennuyer, Nathalie,Beucher-Gaudin, Monique,Zanirato, Ghislaine,Géant, Anne,Staels, Bart,Ktorza, Alain,Farce, Amaury,Caignard, Daniel-Henri,Berthelot, Pascal,Lebegue, Nicolas
, p. 310 - 326 (2017/06/14)
A series of benzothiazol-2-one containing α-ethoxyphenylpropionic acid derivatives incorporating resveratrol or butein scaffolds were designed as fused full PPARγ agonist ligands and SIRT1-activating compounds for the treatment of type 2 diabetes (T2D) an
Synthesis and evaluation of 2-nonylaminopyridine derivatives as PPAR ligands
Usui, Shinya,Fujieda, Hiroki,Suzuki, Takayoshi,Yoshida, Naoaki,Nakagawa, Hidehiko,Ogura, Michitaka,Makishima, Makoto,Miyata, Naoki
, p. 1053 - 1059 (2008/02/12)
To find novel PPAR ligands, we prepared several 3-{3 or 4-[2-(nonylpyridin-2-ylamino)ethoxy]phenyl}-propanoic acid derivatives which were designed based on the structure of our previous PPARγ ligand 1. In PPAR binding affinity assays, compound 4, which ha
SUBSTITUTED CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT OF DIABETES AND LIPID DISORDERS, THEIR PREPARATION AND USE
-
Page/Page column 15-16, (2008/06/13)
The present invention is concerned with racemic or enantiomerically enriched substituted carboxylic acids and derivatives thereof represented by Formula 1 ; or pharmaceutically acceptable salts thereof. The present invention also includes pharmaceutical c
Novel thieno oxazine analogues as antihyperglycemic and lipid modulating agents
Das, Saibal Kumar,Reddy, K. Anantha,Abbineni, Chandrasekhar,Iqbal, Javed,Suresh,Premkumar,Chakrabarti, Ranjan
, p. 399 - 403 (2007/10/03)
A series of phenyl acetic acid and α-hydroxy propionic acid derivatives were synthesized. In vivo studies of the compounds indicated compound 2c as the most potent in one of the series, which has both glucose and lipid lowering properties. The syntheses and biological studies have been discussed.
Tricyclic compounds and their use in medicine: process for their preparation and pharmaceutical compositions containing them
-
, (2008/06/13)
A compound of formula (1) it derivatives, its analogs, its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, or its pharmaceutically acceptable solvates, processes for its preparation and methods of use thereof.
Novel tricyclic-α-alkyloxyphenylpropionic acids: Dual PPARα/γ agonists with hypolipidemic and antidiabetic activity
Sauerberg, Per,Pettersson, Ingrid,Jeppesen, Lone,Bury, Paul S.,Mogensen, John P.,Wassermann, Karsten,Brand, Christian L.,Sturis, Jeppe,W?ldike, Helle F.,Fleckner, Jan,Andersen, Anne-Sofie T.,Mortensen, Steen B.,Svensson, L. Anders,Rasmussen, Hanne B.,Lehmann, S?ren V.,Polivka, Zdenek,Sindelar, Karel,Panajotova, Vladimira,Ynddal, Lars,Wulff, Erik M.
, p. 789 - 804 (2007/10/03)
Synthesis and structure-activity relationships of tricyclic α-ethoxy-phenylpropionic acid derivatives guided by in vitro PPARα and PPARγ transactivation data and computer modeling led to the identification of the novel carbazole analogue, 3q, with and dual PPARα (EC50 = 00.36 μM) and PPARγ (EC50 = 0.17 μM) activity in vitro. Ten days treatment of db/db mice with 3q improved the insulin sensitivity, as measured by OGTT, better than that seen with both pioglitazone and rosiglitazone treatment, suggesting in vivo PPARγ activity. Likewise, 3q lowered plasma triglycerides and cholesterol in high cholesterol fed rats after 4 days treatment, indicating in vivo PPARα activity. Investigations of the pharmacokinetics of selected compounds suggested that extended drug exposure improved the in vivo activity of in vitro active compounds.
Tricyclic compounds and their use in medicine process for their preparation and pharmaceutical compositions containing them
-
, (2008/06/13)
Novel beta -aryl- alpha -oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them. The compounds have hypolipidemic, antihyperglycemic uses.
