ArticleChemMedChem2009
Synthesis, structural analysis, and biological evaluation of thioxoquinazoline derivatives as phosphodiesterase 7 inhibitors.
Article in ChemMedChem, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed.
- Synthesis, in vitro and in silico evaluation of quinazoline and triazoloquinazoline derivatives as PDE7A inhibitors.Research in pharmaceutical sciences · 2026Article
- From 2-Azido Products to Complex Nitrogen Heterocycles: The Versatile Ugi MCR in Modern Synthesis.Current organic synthesis · 2026Article
- New quinazoline derivatives with anti-inflammatory activity and computationally predicted PDE7A binding: synthesis, molecular modeling, andFrontiers in pharmacology · 2026Article
- Chemical Space Exploration and Machine Learning-Based Screening of PDE7A Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Recent Advances in Medicinal Chemistry of Phosphodiesterase 7 Inhibitors and their Potential Therapeutic Applications.Recent advances in inflammation & allergy drug discovery · 2025Review
- Phosphodiesterase 7: a potential novel therapeutic target in ovarian cancer.Frontiers in pharmacology · 2025Article
- Design, synthesis, molecular docking, and molecular dynamic studies of novel quinazoline derivatives as phosphodiesterase 7 inhibitors.Frontiers in pharmacology · 2024Article
- Inhaled Phosphodiesterase Inhibitors for the Treatment of Chronic Obstructive Pulmonary Disease.Drugs · 2021Review
- Improved Controlled Release and Brain Penetration of the Small Molecule S14 Using PLGA Nanoparticles.International journal of molecular sciences · 2021Article
- Role of Phosphodiesterase 7 (PDE7) in T Cell Activity. Effects of Selective PDE7 Inhibitors and Dual PDE4/7 Inhibitors on T Cell Functions.International journal of molecular sciences · 2020Review
- Cyclic Nucleotide-Specific Phosphodiesterases as Potential Drug Targets for Anti-Leishmania Therapy.Antimicrobial agents and chemotherapy · 2018Article
- Amyloid β-induced impairments on mitochondrial dynamics, hippocampal neurogenesis, and memory are restored by phosphodiesterase 7 inhibition.Alzheimer's research & therapy · 2018Article
- Promoting in vivo remyelination with small molecules: a neuroreparative pharmacological treatment for Multiple Sclerosis.Scientific reports · 2017Article
- Phosphodiesterase 7 inhibition induces dopaminergic neurogenesis in hemiparkinsonian rats.Stem cells translational medicine · 2015Article
- Crosstalk between phosphodiesterase 7 and glycogen synthase kinase-3: two relevant therapeutic targets for neurological disorders.ACS chemical neuroscience · 2014Article
- Comparative assessment of PDE 4 and 7 inhibitors as therapeutic agents in experimental autoimmune encephalomyelitis.British journal of pharmacology · 2013Article
- Inhibition of endogenous phosphodiesterase 7 promotes oligodendrocyte precursor differentiation and survival.Cellular and molecular life sciences : CMLS · 2013Article
- Identification in silico and experimental validation of novel phosphodiesterase 7 inhibitors with efficacy in experimental autoimmune encephalomyelitis mice.ACS chemical neuroscience · 2012Article
- Cyclic nucleotide phosphodiesterase (PDE) isozymes as targets of the intracellular signalling network: benefits of PDE inhibitors in various diseases and perspectives for future therapeutic developments.British journal of pharmacology · 2012Review
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Corrections and comments
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Authors and funding
15 authors.
Funding
Abstract
PDE7 inhibitors regulate pro-inflammatory and immune T-cell functions, and are a potentially novel class of drugs especially useful in the treatment of a wide variety of immune and inflammatory disorders. Starting from our lead family of thioxoquinazolines, we designed, synthesized, and characterized a novel series of thioxoquinazoline derivatives. Many of these compounds showed inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7A1 and at the micromolar level against PDE4D2. Cell-based studies showed that these compounds not only increased intracellular cAMP levels, but also had interesting anti-inflammatory properties within a therapeutic window. The in silico data predict that these compounds are capable of the crossing the blood-brain barrier. The X-ray crystal structure of the PDE7A1 catalytic domain in complex with compound 15 at a resolution of 2.4 A demonstrated that hydrophobic interactions at the active site pocket are a key feature. This structure, together with molecular modeling, provides insight into the selectivity of the PDE inhibitors and a template for the discovery of new PDE7 or PDE7/PDE4 dual inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.