244152-94-1Relevant articles and documents
Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists
Zhang, Hao,Ding, Charles Z.,Lai, Zhi,Chen, Sean S.,Devasthale, Pratik,Herpin, Tim,Morton, George,Qu, Fucheng,Ryono, Denis,Smirk, Rebecca,Wang, Wei,Wu, Shung,Ye, Xiang-Xang,Li, Yi-Xin,Apedo, Atsu,Farrelly, Dennis,Wang, Tao,Gu, Liqun,Morgan, Nathan,Flynn, Neil,Chu, Cuixia,Kunselman, Lori,Lippy, Jonathan,Locke, Kenneth,O'Malley, Kevin,Harrity, Thomas,Cap, Michael,Zhang, Lisa,Hosagrahara, Vinayak,Kadiyala, Pathanjali,Xu, Carrie,Doweyko, Arthur M.,Zahler, Robert,Hariharan, Narayanan,Cheng, Peter T.W.
, p. 1196 - 1205 (2015/04/27)
The design, synthesis and structure-activity relationships of a novel series of 3,4-disubstituted pyrrolidine acid analogs as PPAR ligands is outlined. In both the 1,3- and 1,4-oxybenzyl pyrrolidine acid series, the preferred stereochemistry was shown to be the cis-3R,4S isomer, as exemplified by the potent dual PPARα/γ agonists 3k and 4i. The N-4-trifluoromethyl-pyrimidinyl pyrrolidine acid analog 4i was efficacious in lowering fasting glucose and triglyceride levels in diabetic db/db mice.
Discovery of tertiary aminoacids as dual PPARα/γ agonists-I
Devasthale, Pratik V.,Chen, Sean,Jeon, Yoon,Qu, Fucheng,Ryono, Denis E.,Wang, Wei,Zhang, Hao,Cheng, Lin,Farrelly, Dennis,Golla, Rajasree,Grover, Gary,Ma, Zhengping,Moore, Lisa,Seethala, Ramakrishna,Sun, Wei,Doweyko, Arthur M.,Chandrasena, Gamini,Sleph, Paul,Hariharan, Narayanan,Cheng, Peter T.W.
, p. 2312 - 2316 (2008/02/01)
A novel series of potent dual agonists of PPARα and PPARγ, the alkoxybenzylglycines, was identified and explored using a solution-phase library approach. The synthesis and structure-activity relationships of this series of dual PPARα/γ agonists are descri
Antihyperglycemic activity of new 1,2,4-oxadiazolidine-3,5-diones
Malamas, Michael S,Sredy, Janet,McCaleb, Michael,Gunawan, Iwan,Mihan, Brenda,Sullivan, Donald
, p. 31 - 42 (2007/10/03)
A series of 1,2,4-oxadiazolidine-3,5-diones was synthesized and evaluated as oral antihyperglycemic agents in the obese insulin resistant db/db and ob/ob mouse - the two models for Type 2 diabetes mellitus. The majority of the prepared methoxy- and ethoxy-linked oxazole 1,2,4-oxadiazolidine-3,5-diones normalized plasma glucose levels at the 100 mg kg-1 oral dose in the db/db diabetic mouse model, and several amongst them reduced the glucose levels at the 20 mg kg-1 oral dose. The most potent compounds in the db/db mouse model were also active in the ob/ob mouse model normalizing the plasma glucose levels at the 20 mg kg-1 oral dose. The trifluoromethoxy analog 32 was the most active compound of the series, reducing significantly the plasma glucose levels at the 5 mg kg-1 oral dose. Oxadiazole-tailed 1,2,4-oxadiazolidine-3,5-diones were also active in both the db/db and ob/ob diabetic mouse models normalizing plasma glucose levels at the 100 mg kg-1 oral dose.
