53585-95-8Relevant articles and documents
Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD)
Lagu, Bharat,Kluge, Arthur F.,Tozzo, Effie,Fredenburg, Ross,Bell, Eric L.,Goddeeris, Matthew M.,Dwyer, Peter,Basinski, Andrew,Senaiar, Ramesh S.,Jaleel, Mahaboobi,Tiwari, Nirbhay Kumar,Panigrahi, Sunil K.,Krishnamurthy, Narasimha Rao,Takahashi, Taisuke,Patane, Michael A.
supporting information, p. 935 - 940 (2018/09/06)
The X-ray structure of the previously reported PPARδ modulator 1 bound to the ligand binding domain (LBD) revealed that the amide moiety in 1 exists in the thermodynamically disfavored cis-amide orientation. Isosteric replacement of the cis-amide with five-membered heterocycles led to the identification of imidazole 17 (MA-0204), a potent, selective PPARδ modulator with good pharmacokinetic properties. MA-0204 was tested in vivo in mice and in vitro in patient-derived muscle myoblasts (from Duchenne Muscular Dystrophy (DMD) patients); 17 altered the expression of PPARδ target genes and improved fatty acid oxidation, which supports the therapeutic hypothesis for the study of MA-0204 in DMD patients.
Chiral Amino Alcohol Accelerated and Stereocontrolled Allylboration of Iminoisatins: Highly Efficient Construction of Adjacent Quaternary Stereogenic Centers
Tan, Qiuyuan,Wang, Xinqiao,Xiong, Yang,Zhao, Zimeng,Li, Lu,Tang, Pei,Zhang, Min
supporting information, p. 4829 - 4833 (2017/04/11)
We have developed a highly efficient asymmetric allylboration of ketimines with nonchiral γ,γ-disubstituted allylboronic acids by using a chiral amino alcohol as the directing group, which is otherwise challenging. The amino alcohol not only serves as a cheap source of nitrogen and chirality, but also dramatically enhances the reactivity. The versatility of this method was demonstrated by its ability to access all four stereoisomers with adjacent quaternary carbon centers. A reaction model was proposed to explain the diastereoselectivity and the rate-accelerating effect.
A convergent synthesis of mycophenolic acid
Ple, Patrick A.,Hamon, Annie,Jones, Geraint
, p. 3395 - 3400 (2007/10/03)
A new method for the synthesis of Mycophenolic acid using a convergent approach has been developed where the key step is a palladium mediated allyl-aryl tin coupling.