Ultrasound One Pot Synthesis of Fused Quinazolinones and Quinazolinediones, Screening and Molecular Docking Study as Phosphodiesterase 7A Inhibitors | ||
| Egyptian Journal of Chemistry | ||
| Article 9, Volume 62, Issue 8, August 2019, Pages 1451-1466 PDF (1.59 M) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2019.7130.1587 | ||
| Authors | ||
| sherin Elfeky* 1; Tariq Sobahi2; Magdy M Gineinah3; Nesreen S Ahmed4 | ||
| 1Department of Pharmaceutical organic chemistry, Faculty of Pharmacy, Mansoura University,Egypy | ||
| 2king abdulaziz university, Jeddah, faculty of science | ||
| 3king abdulaziz university, Jeddah, faculty of Pharmacy | ||
| 4Department of Medicinal Chemistry, National Research Center, Cairo, Egypt | ||
| Abstract | ||
| Phosphodiesterase 7A enzyme is one the most recent targets for designing potent anti-inflammatory agents with minimal side effects. Quinazolinones are unique building blocks of wide biological activities. Different Quinazolinones were reported to act as Phosphodiesterase 7A inhibitors anti-inflammatory particularly against choronic inflammation and autoimmune disease. Ultrasound is a green convenient method for synthesis of different heterocyclic ring system that is advantageous in terms of yield and reaction time. Ultrasound was used for one pot synthesis of 3-substituted 6-aryl-dihydroisoindolo[2,1-a]quinazoline-5,11-diones and 3-Aryl quinazoline-2,4(1H,3H)-diones. Seventeen compounds were synthesized in good yields. The synthesized compounds were inspected for in vitro inhibitory activity against phosphodiesterase7A enzyme. Molecular docking was used to study the mode of interaction of all the synthesized compounds into the enzyme phosphodiesterase 7A binding site. Five compounds showed high inhibitory activity of enzyme Phosphodiesterase 7A at micro-molar level compared to reference drug. The compounds showed good recognition at the enzyme binding site in the molecular docking. There was a good agreement between the molecular docking and the biological screening results. | ||
| Keywords | ||
| Docking study; Phosphodiesterase 7A inhibitory assay; In vitro screening; Quinazolinedione; Dihydroisoindoloquinazolinone | ||
|
Statistics Article View: 666 PDF Download: 568 |
||
