477546-90-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor α and γ dual agonists
Suh, Young-Ger,Kim, Nam-Jung,Koo, Bon-Woong,Lee, Kwang-Ok,Moon, Sung-Hyun,Shin, Dong-Hyung,Jung, Jong-Wha,Paek, Seung-Mann,Chang, Dong-Jo,Li, Funan,Kang, Hyun-Jin,Le, Tuong Vy Thi,Yu, Na Chae,Chang, Yell Shin,Kim, Mi-Kyung,Joong, In Lim,Ryu, Jae-Sang,Park, Hyun-Ju
experimental part, p. 6318 - 6333 (2009/11/30)
In an effort to develop dual PPARα/γ activators with improved therapeutic efficacy, a series of diaryl α-ethoxy propanoic acid compounds comprising two aryl groups linked by rigid oxime ether or isoxazoline ring were designed and synthesized and their biological activities were examined. Most of the compounds possessing an oxime ether linker were more potent PPARγ activators than the lead PPARα/γ dual agonist, tesaglitazar in vitro. Compound 18, one of the derivatives with an oxime ether linker, was found to selectively transactivate PPARγ (EC50 = 0.028 μM) over PPARα (EC50 = 7.22 μM) in vitro and lower blood glucose in db/db mice more than muraglitazar after oral treatment for 11 days.
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARα/γ dual agonists
Kim, Nam-Jung,Lee, Kwang-Ok,Koo, Bon-Woong,Li, Funan,Yoo, Ja-Kyung,Park, Hyun-Ju,Min, Kyung-Hoon,Lim, Joong In,Kim, Mi Kyung,Kim, Jin-Kwan,Suh, Young-Ger
, p. 3595 - 3598 (2008/02/11)
We have developed a new class of PPARα/γ dual agonists, which show excellent agonistic activity in PPARα/γ transactivation assay. In particular, (R)-9d was identified as a potent PPARα/γ dual agonist with EC50s of 0.377 μM in PPARα and 0.136 μM in PPARγ, respectively. Interestingly, the structure-activity relationship revealed that the stereochemistry of the identified PPARα/γ dual agonists significantly affects their agonistic activities in PPARα than in PPARγ.
Phenylalkyloxy-phenyl derivatives
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, (2008/06/13)
The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.
2-ETHOXY-3-PHENYLPROPIONIC ACID DERIVATIVES FOR THE TREATMENT OF LIPID DISORDERS
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Page 19, (2008/06/13)
A compound of formula (I) wherein T represents O, S or NR and wherein R represents a H, a C1-6alkyl group or a phenyl C1-6alkyl group and pharmaceutically acceptable salts thereof, processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and and pharmaceutical compositions containing them.
