2. Academic Validation
  3. Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists

Design and synthesis of the first generation of dithiolane thiazolidinedione- and phenylacetic acid-based PPARgamma agonists

  • J Med Chem. 2006 Jul 13;49(14):4072-84. doi: 10.1021/jm0510880.
Amar G Chittiboyina 1,  Meenakshi S Venkatraman,  Cassia S Mizuno,  Prashant V Desai,  Akshay Patny,  Stephen C Benson,  Christopher I Ho,  Theodore W Kurtz,  Harrihar A Pershadsingh,  Mitchell A Avery
Affiliations

Affiliation

  • 1 Laboratory for Applied Drug Design and Synthesis, Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi, 38677, USA.
PMID: 16821769 DOI: 10.1021/jm0510880
Abstract

A series of novel derivatives of potent antioxidant vitamin, alpha-lipoic acid, and related analogues were designed, synthesized, and evaluated for their PPARgamma agonist activities. Compounds 9a and the water soluble analogue11e were found to be potent PPARgamma 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.

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