Design, synthesis, molecular docking, and molecular dynamic studies of novel quinazoline derivatives as phosphodiesterase 7 inhibitors

AA El-Malah, MM Gineinah, MT Khayat… - Frontiers in …, 2024 - frontiersin.org
Introduction: Phosphodiesterase 7 (PDE7) is a high-affinity cyclic AMP (cAMP)-specific PDE
that is expressed in immune and proinflammatory cells. In this work, we explore the …

Synthesis, structural analysis, and biological evaluation of thioxoquinazoline derivatives as phosphodiesterase 7 inhibitors

T Castaño, H Wang, NE Campillo… - ChemMedChem …, 2009 - Wiley Online Library
PDE7 inhibitors regulate pro‐inflammatory and immune T‐cell functions, and are a
potentially novel class of drugs particularly useful for treatment of a wide variety of immune …

Design, Synthesis, and Structure− Activity Relationship, Molecular Modeling, and NMR Studies of a Series of Phenyl Alkyl Ketones as Highly Potent and Selective …

S Zheng, G Kaur, H Wang, M Li… - Journal of medicinal …, 2008 - ACS Publications
Phosphodiesterase 4 catalyzes the hydrolysis of cyclic AMP and is a target for the
development of anti-inflammatory agents. We have designed and synthesized a series of …

Structural optimization and bioactivity evaluation of 2-(Methylcarbonylamino) thiazole derivatives as novel PDE4B inhibitors

R Ma, N Song, X Gu, R Guo, M Shen, S Zhang, W Yang… - Tetrahedron, 2024 - Elsevier
Abstract Phosphodiesterase-4 (PDE4) is a protease belonging to the phosphodiesterase
family, with a specific function of hydrolyzing intracellular cyclic adenosine monophosphate …

Synthesis, docking and anti-inflammatory activity of triazole amine derivatives as potential phosphodiesterase-4 inhibitors

A SinghGrewal, V Lather, D Pandita… - Anti-Inflammatory & Anti …, 2017 - ingentaconnect.com
Background: Phosphodiesterase 4 (PDE4), is one of the members of PDE superfamily which
catalyzes the hydrolysis of cyclic adenosine monophosphate to adenosine monophosphate …

Design, synthesis, and pharmacological characterization of some 2‐substituted‐3‐phenyl‐quinazolin‐4(3H)‐one derivatives as phosphodiesterase inhibitors

KM Amin, GH Hegazy, RF George… - Archiv der …, 2021 - Wiley Online Library
Abstract Some 3‐phenyl‐quinazolin‐4 (3H)‐one‐2‐thioethers (3a–e, 5a, b, 7a–e, 9a–d, 10a–
d, and 12) along with 2‐aminoquinazoline derivatives 13a–c were prepared and screened …

Triazole‐Pyridine Dicarbonitrile Targets Phosphodiesterase 4 to Induce Cytotoxicity in Lung Carcinoma Cells

HK Keerthy, S Mohan, Basappa… - Chemistry & …, 2019 - Wiley Online Library
Abstract Phosphodiesterase 4 (PDE4) is a key enzyme involved in the hydrolysis of cyclic
adenosine monophosphate (cAMP) and widely expressed in several types of cancers. The …

A search for antiinflammatory therapies: Synthesis, in silico investigation of the mode of action, and in vitro analyses of new quinazolin‐2, 4‐dione derivatives targeting …

AH Abdelmonsef, MA Abdelhakeem… - Journal of …, 2022 - Wiley Online Library
Inflammation is the response of the body's immune system to harmful stimuli. The expression
of phosphodiesterase 4 enzyme (PDE4) was demonstrated in many inflammatory cells …

Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: design, synthesis, and structure-activity relationship study of …

ZZ Zhou, BC Ge, QP Zhong, C Huang, YF Cheng… - European Journal of …, 2016 - Elsevier
In this study, catecholamides (7a–l) bearing different aromatic rings (such as pyridine-2-yl,
pyridine-3-yl, phenyl, and 2-chlorophenyl groups) were synthesized as potent …

Discovery and optimization of 4-(imidazo[1,2-a]pyrimidin-3-yl)thiazol-2-amine derivatives as novel phosphodiesterase 4 inhibitors

Z Wu, F Zhang, Z Chen, X Wang, X Liu, G Yang… - Molecular Diversity, 2024 - Springer
Phosphodiesterases (PDEs) are important intracellular enzymes that hydrolyze the second
messengers cAMP and/or cGMP. Now several studies have shown that PDE4 received …