Publications
Design and construction of novel pyridinepyrimidine hybrids as selective COX-2 suppressors: anti-inflammatory potential, ulcerogenic profile, molecular modeling and ADME/Tox studies
Deep insights into the Cu- and W-doped Na0.5Bi0.5TiO3 solid solution: A study focusing on optical, dielectric and electrical properties
Discovery of Potent Indolyl-Hydrazones as Kinase Inhibitors for Breast Cancer: Synthesis, X-ray Single-Crystal Analysis, and In Vitro and In Vivo Anti-Cancer Activity Evaluation
Design, synthesis, and biological evaluation of indole-2-carboxamides as SARS CoV-2 main protease inhibitors
Design, synthesis, characterization, spectral, chemical analysis, biological evaluation, and molecular docking studies of novel fatty Schiff base ligands and their nickel and mercury complexes
Digital Health Interventions for Promoting Healthy Aging: A Systematic Review of Adoption Patterns, Efficacy, and User Experience
Design, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents
Design and construction of novel pyridine-pyrimidine hybrids as selective COX-2 suppressors: anti-inflammatory potential, ulcerogenic profile, molecular modeling and ADME/Tox studies
Dynamical and physical characteristics of soliton solutions to the (2+1)-dimensional Konopelchenko-Dubrovsky system
Development of Soft Luliconazole Invasomes Gel for Effective Transdermal Delivery: Optimization to In-Vivo Antifungal Activity
Design and Performance Evaluation of a Novel Metamaterial Broadband THz Filter for 6G Applications
Diagnosis of patellofemoral osteoarthritis using enhanced sequential deep learning techniques
Design and performance evaluation of a novel metamaterial broadband THz filter for 6G applications
Design and performance evaluation of a novel metamaterial broadband THz filter for 6G applications
Dual activity of indolin-2-ones containing an arylidene motif: DNA and BSA interaction
Dual activity of indolin-2-ones containing an arylidene motif: DNA and BSA interaction
Developing Physical Therapy Students’ Medical Report Writing Skills During COVID-19: A TPACK Based ESP Course.
Dynamics of two-qubit Heisenberg XY state: external magnetic field and intrinsic decoherence effects
Development of Artificial Intelligence Based Safety Performance Measures for Urban Roundabouts
Dual activity of indolin-2-ones containing an arylidene motif: DNA and BSA interaction
Discovery of new 5-substituted-indole-2- carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action
Design of biosensor for synchronized identification of diabetes using deep learning
Design, synthesis, and biological evaluation of indole-2-carboxamides as SARS CoV-2 main protease inhibitors
Design, synthesis, and biological evaluation of indole-2-carboxamides as SARS CoV-2 main protease inhibitors
Design, Synthesis, and Biological Evaluation of New Indole-2-Carboxamides as Anti-Coronaviral Agents Targeting SARS CoV-2 Main Protease inhibitors
Deep learning-enhanced diabetic retinopathy image classification
Design, synthesis, docking and mechanistic studies of new thiazolyl/thiazolidinylpyrimidine-2,4-dione antiproliferative agents
Data Protection in IoT using CoAP based on Enhanced DTLS
Diagnosis of patellofemoral osteoarthritis using enhanced sequential deep learning techniques
Direct synthesis of sodium doped Cu2O/GO nanocomposites for catalytic hydrogen production from NaBH4
Discovery of Novel Tetramethylpyrazine Containing Chalcone Derivatives as Anti-Inflammatory Agents
Designing a Graphene Metasurface Organic Material Sensor for Detection of Organic Compounds in Wastewater
Designing of Graphene Meta-surface Organic Material Sensor for Detection of Organic Compounds in Wastewater (Sh)
Design, synthesis and antimicrobial activity of novel quinoline- 2-one hybrids as promising DNA gyrase and topoisomerase IV inhibitors
Dosimetric characterization of CyberKnife® robotic SRS using MOSFET-based "MOskin" detector
Does Financial Development Really Improve Environmental Quality in Al-Jouf Region? Empirical Contribution to the Environmental Politics
Development of Olive Oil Containing Phytosomal Nanocomplex for Improving Skin Delivery of Quercetin: Formulation Design Optimization, In Vitro and Ex Vivo Appraisals
Distinctive spectroscopic features of samarium ions in the lithium zinc-borate glass
Deep learning models for multilabel ECG abnormalities classification: A comparative study using TPE optimization
Direct synthesis of sodium doped Cu2O/GO nanocomposites for catalytic hydrogen production from NaBH4
Dynamo script and a BIM-based process for measuring embodied carbon in buildings during the design phase
Design, Synthesis and Biological Evaluation of Syn and Anti-like Double Warhead Quinolinones Bearing Dihydroxy Naphthalene Moiety as Epidermal Growth Factor Receptor Inhibitors with Potential Apoptotic Antiproliferative Action
Design, Synthesis, and Anti-Proliferative Action of Purine/Pteridine-Based Derivatives as Dual Inhibitors of EGFR and BRAFV600E
Design, synthesis, docking and mechanistic studies of new thiazolyl/thiazolidinylpyrimidine-2,4-dione antiproliferative agents
Development of Olive Oil Containing Phytosomal Nanocomplex for Improving Skin Delivery of Quercetin: Formulation Design Optimization, In Vitro and Ex Vivo Appraisals
Discovery of new 5-substituted-indole-2- carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action
Detection and Selective Removal Strategy of Thorium Ions Using a Novel Fluorescent Ligand and Hybrid Mesoporous γ-Al2O3-like Nanoneedles
Development of Bi2O3/MoSe2 mixed nanostructures for photocatalytic degradation of methylene blue dye
Diagnosing Melanomas in Dermoscopy Images Using Deep Learning
Development of a Smart Signalization for Emergency Vehicles
Design and construction of novel pyridine-pyrimidine hybrids as selective COX-2 suppressors: anti-inflammatory potential, ulcerogenic profile, molecular modeling and ADME/Tox studies Mohamed E. Shaker,Hesham A. M. Goma,Izzeddin Alsalahat,Nadia A. A. Elkanzi,Amany A. Azouz,Mohamed Sadek Abdel-Bakky, show all Pages 1804-1817 | Received 10 May 2023, Accepted 27 Nov 2023, Published online: 28 Dec 2023 Cite this article https://doi.org/10.1080/07391102.2023.2293257 CrossMark LogoCrossMark Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days Full Article Figures & data References Supplemental Citations Metrics Reprints & Permissions Read this article Abstract NSAIDs represent a mainstay in pain and inflammation suppression, and their actions are mainly based on inhibiting COX-1 and COX-2 enzymes. Due to the adverse effects of these drugs, especially on the stomach and heart, scientists efforts have been directed to manufacture selective COX-2 without cardiovascular side effects and with minimal effects on the stomach. The cardiovascular side effects are thought to be related to the chemical composition rather than mechanism of action of these drugs. Novel pyridopyrimidines, 9a-j, were prepared and their chemical structures were confirmed by NMR, mass and IR Spectra, and elemental analysis. The effect of the 9a-j compounds on COX-1 and COX-2 was assessed and it was found that 2-hydrazino-5-(4-methoxyphenyl)-7-phenyl-3H-pyrido[2,3-d)pyrimidin-4-one (9d) was the most potent COX-2 inhibitor (IC50 = 0.54 uM) compared to celecoxib (IC50 = 1.11 uM) with selectivity indices of 6.56 and 5.12, respectively. The in vivo inhibition of paw edema of novel compounds 9a-j was measured using carrageenan-induced paw edema method, and that 2-hydrazino-5-(4-methoxyphenyl)-7-phenyl-3H-pyrido[2,3-d)pyrimidin-4-one (9d) showed the best inhibitory activity in comparison with the other compounds and celecoxib. The gastroprotective effect of the potent derivatives 9d, 9e, 9f, 9 g and 9h was investigated. 2-Hydrazino-5-(4-methoxyphenyl)-7-phenyl-3H-pyrido[2,3-d)pyrimidin-4-one (9d) and 7-(chlorophenyl)-hydrazino-5-(4-methoxyphenyl)-3H-pyrido[2,3-d)pyrimidin-4-one (9e) showed ulcer indices comparable to celecoxib (1 and 0.5 vs 0.5, respectively). Docking studies were carried out and they confirmed the mechanistic action of the designed compounds Keywords: COXs inhibitorsanti-inflammatorycelecoxibNSAIDspyridopyrimidines Disclosure statement No potential conflict of interest was reported by the author(s). Additional information Funding This research was funded by the Deanship of Scientific Research at Jouf University, Saudi Arabia through a research grant group to ME Shaker (DSR-2022-RG-0149). Share Related research People also read Recommended articles Cited by 5 Information for Authors R&D professionals Editors Librarians Societies Open access Overview Open journals Open Select Dove Medical Press F1000Research Opportunities Reprints and e-prints Advertising solutions Accelerated publication Corporate access solutions Help and information Help and contact Newsroom All journals Books Keep up to date Register to receive personalised research and resources by email Sign me up Taylor and Francis Group Facebook pageTaylor and Francis Group X Twitter pageTaylor and Francis Group Linkedin page Taylor and Francis Group Youtube pageTaylor and Francis Group Weibo page Copyright © 2025Informa UK Limited Privacy policy Cookies Terms & conditions Accessibility Registered in England & Wales No. 01072954 5 Howick Place | London | SW1P 1WG Taylor and Francis Group PDF Help
Design, Synthesis, and antiproliferative action of purine/pteridine-based derivatives as dual inhibitors of EGFR and BRAFV600E
Detection and Quantification of Some Ethanol-Producing Bacterial Strains in the Gut of Mouse Model of Non-Alcoholic Fatty Liver Disease: Role of Metformin
Development of Split Ring Resonator Shaped Six Element 2× 3 Multiple Input Multiple Output Antenna for the C/X/Ku/K Band Applications
Development of Split Ring Resonator Shaped Six Element 2 × 3 Multiple Input Multiple Output Antenna for the C/X/Ku/K Band Applications
Dataset of companies’ profitability, government debt, financial statements' key indicators and earnings in an emerging market: Developing a panel and time series database of value-added tax rate increase impacts
Design of Continuous Finite-Time Controller Based on Adaptive Tuning Approach for Disturbed Boost Converters
Development of Forskolin and rutin-loaded polymeric nanoparticles for enhancement of topical ocular delivery: Optimization, in-vitro, ex-vivo, and toxicity evaluation
Development of olive oil containing phytosomal nanocomplex for improving skin delivery of quercetin: formulation design optimization, in vitro and ex vivo appraisals
Development of olive oil containing phytosomal nanocomplex for improving skin delivery of quercetin: formulation design optimization, in vitro and ex vivo appraisals
Design, Synthesis, Docking Study of Pyrazolohydrazinopyrimidin‐4‐one Derivatives and Their Application as Antimicrobials
Development and assessment of phospholipid-based luteolin-loaded lipid nanocapsules for skin delivery
Design, Synthesis, Molecular Modeling, and Anticancer Evaluation of New VEGFR-2 Inhibitors Based on the Indolin-2-One Scaffold
Do learning style preferences influence the cumulative gross point average and self directed learning hours in dental students: a preliminary study
Does Education Sector Improve Environmental Quality in Saudi Arabia?
Designing of Thiophene [3, 2-b] Pyrrole Ring-Based NFAs for High-Performance Electron Transport Materials: A DFT Study
Discovery of new 5-substituted-indole-2- carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action
Discovery of new 5-substituted-indole-2-carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action
Deep Learning-based prediction of Diabetic Retinopathy using CLAHE and ESRGAN for Enhancement
DC pulsed plasma magnetron sputtering of CdO/Cu/CdO multilayers thin films for self-cleaning and optoelectronic applications
Development of Bi2O3/MoSe2 mixed nanostructures for photocatalytic degradation of methylene blue dye
Development of more potent anti microbial drugs from extracts of fve medicinal plants resistant to S. aureus in human fuids: an ex vivo and in vivo analysis
Do learning style preferences influence the cumulative gross point average and self directed learning hours in dental students: a preliminary study
Discovery of new 5-substituted-indole-2- carboxamides as dual epidermal growth factor receptor (EGFR)/cyclin dependent kinase-2 (CDK2) inhibitors with potent antiproliferative action
Development of Bi2O3/MoSe2 mixed nanostructures for photocatalytic degradation of methylene blue dye
Development of Bi2O3/MoSe2 mixed nanostructures for photocatalytic degradation of methylene blue dye
DFFMD: A Deepfake Face Mask Dataset for Infectious Disease Era With Deepfake Detection Algorithms
Development of Smart Mobility Infrastructure in Saudi Arabia: A Benchmarking Approach
Development of Isopropyl-Tailed Chalcones as a New Class of Selective MAO-B Inhibitors for the Treatment of Parkinson’s Disorder
Dual action of epigallocatechin-3-gallate in virus-induced cell Injury
Design technique to mitigate unwanted coupling in densely packed radiating elements of an antenna array for electronic devices and wireless communication systems operating in the millimeter-wave band
Design and fabrication of compact, multiband, and high gain, high isolation, metamaterial-based MIMO antennas for Wire-less Communication Systems
Design and Fabrication of Compact, Multiband, High Gain, High Isolation, Metamaterial-Based MIMO Antennas for Wireless Communication Systems
Design and Fabrication of Compact, Multiband, High Gain, High Isolation, Metamaterial-Based MIMO Antennas for Wireless Communication Systems
Design, synthesis and antimicrobial activity of novel quinoline-2-one hybrids as promising DNA gyrase and topoisomerase IV inhibitors
Discovering Gummadiol and Isoarboreol aspotential inhibitors of sphingosine kinase1: virtual screening and MD simulationstudi
Diagnosis and Stratification of COVID-19 Infections Using Differential Plasma Levels of D-Dimer: A Two-Center Study from Saudi Arabia
Discovering Gummadiol and Isoarboreol as potential inhibitors of sphingosine kinase 1: virtual screening and MD simulation studies
Design, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents
Design, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents
Design, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents
Design and Fabrication of a Low-Cost, Multiband and High Gain Square Tooth-Enabled Metamaterial Superstrate Microstrip Patch Antenna
Developing Metal Complexes for Captopril Quantification in Tablets Using Potentiometric and Conductometric Methods