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Updated: Jul 7, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological
Cécile Parmenon1, Jérôme Guillard, Daniel-Henri Caignard
1SPOT-EA3857, UFR des Sciences Pharmaceutiques, 31 Avenue Monge, 37200 Tours, France.
Abstract:
Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a defect in pancreatic beta-cell. Since their discovery three subtypes of Peroxisomes Proliferators Activated Receptors were identified namely PPARalpha, PPARgamma and PPARbeta/(delta). We were interested in designing novel PPARgamma selective agonists and/or dual PPARalpha/gamma agonists. Based on the typical topology of synthetic PPAR agonists, we focused our design approach on 4,4-dimethyl-1,2,3,4-tetrahydroquinoline as novel cyclic tail.
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