196811-03-7Relevant academic research and scientific papers
Synthesis and biological activity of L-tyrosine-based PPARγ agonists with reduced molecular weight
Liu, Kevin G.,Lambert, Millard H.,Ayscue, Andrea H.,Henke, Brad R.,Leesnitzer, Lisa M.,Oliver, Jr., William R.,Plunket, Kelli D.,Xu,Sternbach, Daniel D.,Willson, Timothy M.
, p. 3111 - 3113 (2001)
A series of PPARγ agonists were synthesized from L-tyrosine that incorporated low molecular weight N-substituents. The most potent analogue, pyrrole (4e), demonstrated a Ki of 6.9 nM and an EC50 of 4.7 nM in PPARγ binding and functional assays, respectively. Pyrrole (4e), which is readily synthesized from L-tyrosine methyl ester in four steps, also demonstrated in vivo activity in a rodent model of Type 2 diabetes.
(S)-3-(4-(2-(5-Methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-(piperazin-1-yl)propanoic acid compounds: Synthesis and biological evaluation of dual PPARα/γ agonists
Zhou, Xinbo,Chen, Wei,Xu, Cheng,Fan, Shiyong,Xie, Yunde,Zhong, Wu,Wang, Lili,Li, Song
scheme or table, p. 2605 - 2608 (2010/06/17)
A series of novel, potent PPARα/γ dual agonists were synthesized and appraised. The most potent analogue, compound 2b demonstrated EC50 value of 0.012 ± 0.002 and 0.032 ± 0.01 μM, respectively, for hPPARα and hPPARγ in transactivation assay. Additionally, compound 2b demonstrated good glucose and lipid lowering effect in genetic diabetic (db/db) mice.
TYROSINE DERIVATIVES SUBSTITUTED BY N-PHENYLACRYLOYL AS AGONISTS OF HPPAR ALPHA AND HPPAR GAMA
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Page/Page column 11, (2008/06/13)
The present invention relates to a compound of formula I, racemates, optically active isomers, or pharmaceutically acceptable salts or solvates thereof, and a pharmaceutical composition comprising the compound, the various radicals in the formula I are the same as defined in the claims. The present invention also relates to a process for preparing the compound of formula I and use of said compound in the preparation of a medicament for the treatment of hyperglycemia, dyslipidemia, type II diabetes mellitus including associated diabetic dyslipidemia
Substitued A-Piperazingly Phenylpropionic Acid Derivatives As Hppar Alpha And/Or Hppar Gamma Agonists
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Page/Page column 8-9, (2008/06/13)
The present invention relates to a compound of formula I, racemates, optically active isomers, or pharmaceutically acceptable salts or solvates thereof, and a pharmaceutical composition comprising the compound, the various radicals in the formula I are the same as defined in the claims. The present invention also relates to a process for preparing the compound of formula I and use of said compound in the preparation of a medicament for the treatment of hyperglycemia, dyslipidemia, type II diabetes mellitus including associated diabetic dyslipidemia
N-(2-benzoylphenyl)-L-tyrosine PPARγ agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent
Cobb, Jeff E.,Blanchard, Steven G.,Boswell, Evan G.,Brown, Kathleen K.,Charifson, Paul S.,Cooper, Joel P.,Collins, Jon L.,Dezube, Milana,Henke, Brad R.,Hull-Ryde, Emily A.,Lake, Debra H.,Lenhard, James M.,Oliver Jr., William,Oplinger, Jeffery,Pentti, Mila,Parks, Derek J.,Plunket, Kelli D.,Tong, Wei-Qin
, p. 5055 - 5069 (2007/10/03)
3-{4-[2-(Benzoxazol-2-ylmethylamino)ethoxy]phenyl}-(2S)-((2- benzoylphenyl)amino)propionic acid (1) and (2S)-((2-benzoylphenyl)amino)-3- {4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phenyl}propionic acid (2) are peroxisome proliferator-activated receptor γ
