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Ultrasound One Pot Synthesis of Fused Quinazolinones and Quinazolinediones, Screening and Molecular Docking Study as Phosphodiesterase 7A Inhibitors

Article

Last updated: 01 Jan 2025

Subjects

-

Tags

Organic chemistry

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.

DOI

10.21608/ejchem.2019.7130.1587

Keywords

Docking study, Phosphodiesterase 7A inhibitory assay, In vitro screening, Quinazolinedione, Dihydroisoindoloquinazolinone

Authors

First Name

sherin

Last Name

Elfeky

MiddleName

-

Affiliation

Department of Pharmaceutical organic chemistry, Faculty of Pharmacy, Mansoura University,Egypy

Email

sherin_el_feky@yahoo.com

City

-

Orcid

0000-0002-5774-8007

First Name

Tariq

Last Name

Sobahi

MiddleName

-

Affiliation

king abdulaziz university, Jeddah, faculty of science

Email

drtariq_s@hotmail.com

City

jeddah

Orcid

-

First Name

Magdy

Last Name

Gineinah

MiddleName

M

Affiliation

king abdulaziz university, Jeddah, faculty of Pharmacy

Email

maggineinah@yahoo.com

City

-

Orcid

-

First Name

Nesreen

Last Name

Ahmed

MiddleName

S

Affiliation

Department of Medicinal Chemistry, National Research Center, Cairo, Egypt

Email

nesreen69eg@yahoo.com

City

-

Orcid

0000-0001-9136-9986

Volume

62

Article Issue

8

Related Issue

6668

Issue Date

2019-08-01

Receive Date

2019-01-09

Publish Date

2019-08-01

Page Start

1,451

Page End

1,466

Print ISSN

0449-2285

Online ISSN

2357-0245

Link

https://ejchem.journals.ekb.eg/article_27688.html

Detail API

https://ejchem.journals.ekb.eg/service?article_code=27688

Order

9

Type

Original Article

Type Code

297

Publication Type

Journal

Publication Title

Egyptian Journal of Chemistry

Publication Link

https://ejchem.journals.ekb.eg/

MainTitle

Ultrasound One Pot Synthesis of Fused Quinazolinones and Quinazolinediones, Screening and Molecular Docking Study as Phosphodiesterase 7A Inhibitors

Details

Type

Article

Created At

22 Jan 2023