Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors

Targeting PPAR<i>γ</i> Receptor Using New Phosphazene Derivative Containing Thiazolidinedione: Design, Synthesis, and Glucose Uptake

“…Peroxisome proliferator-activated receptors (PPARs) are known transcription factors that directly control the expression of genes involved in lipid and glucose metabolism [11]. The mechanism of PPARs has been described [12]. Among the Open Journal of Medicinal Chemistry three isotypes of PPARs (PPARα, PPARβ and PPARγ), PPARγ is the most studied for drug discovery.…”

Quinazoline pharmacophore in therapeutic medicine

“…Administration of 3-substitutedquinazolin-2,4-dithione as optimized PDE7 inhibitor improved brain damage and enhanced behavioral aftermath in a permanent middle cerebral artery obstruction (pMCAO) stroke model (Redondo et al, 2012;Susín et al, 2012). Sánchez et al (2013) reported the inhibitory potencies of quinazoline-4-thione 24 at submicromolar levels against the catalytic domain of PDE7. Smallmolecule phosphodiesterase probe investigation established 4-aminoquinazoline 25 as PDE1 inhibitors that readily cross the blood brain barrier (Humphrey et al, 2014).…”

New synthetic route to pyrimido[4,5-g]quinazoline-4,9-diones

“…A direct synthesis of 6 from 3 was also attempted using a pressure reactor in aqueous ammonium hydroxide at 120°C for several days. 25 However, ring closure did not occur due probably to the limited solubility of 3 in the reaction medium. Subsequently the diacid 4, which was prepared in 86% yield by hydrolyzation of 3 with lithium hydroxide, was reacted with formamide at 150°C 26 in order to produce 6, but the target compound was not formed.…”