905990-92-3Relevant academic research and scientific papers
Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARγ agonists
Chittiboyina, Amar G.,Venkatraman, Meenakshi S.,Mizuno, Cassia S.,Desai, Prashant V.,Patny, Akshay,Benson, Stephen C.,Ho, Christopher I.,Kurtz, Theodore W.,Pershadsingh, Harrihar A.,Avery, Mitchell A.
, p. 4072 - 4084 (2007/10/03)
A series of novel derivatives of potent antioxidant vitamin, α-lipoic acid, and related analogues were designed, synthesized, and evaluated for their PPARγ agonist activities. Compounds 9a and the water soluble analogue 11e were found to be potent PPARγ agonists. Compound 9a appeared to have a significant role in improving insulin sensitivity and reducing triglyceride levels in fa/fa rats as well as inhibited proliferation of a variety of normal and neoplastic cultured human cell types. These novel compounds may prove efficacious not only in the treatment of Type 2 diabetes, but also atherosclerosis, prevention of vascular restenosis, and inflammatory skin diseases.
Solid-phase synthesis of hybrid thiazolidinedione-fatty acid PPARγ ligands
Tomkinson, Nicholas C. O.,Sefler, Andrea M.,Plunket, Kelli D.,Blanchard, Steven G.,Parks, Derek J.,Willson, Timothy M.
, p. 2491 - 2496 (2007/10/03)
A library of thiazolidinedione-fatty acid hybrid molecules was designed to probe the relationship between natural and synthetic PPAR ligands. Solid-phase synthesis of the library led to the identification of several high affinity PPARYγ ligands.
