Publications
Resolving Spectral Overlaps in Anti-Parkinson Drug Combinations: A Green Spectrophotometric Approach for Entacapone Determination
One-pot synthesis of Au/GO nanozymes: enhanced catalytic activity via in situ chemical reduction
Pyrazole/pyrimidine derivatives endowed with azobenzenes as dual EGFR T790M and VEGFR-2 inhibitors: anticancer, docking, synthesis, design and ADMET assessments
OpenFieldAI – New Open-Source AI Based Software for Tracking Rodents and Training Open Field Test Models
Chitosan/polyacrylic acid nanogel-mediated delivery system for cancer treatment: Design, synthesis, ADMET, docking of thiazole derivatives as dual inhibitors of VEGFR-2 and EGFRT790M
Ferulic acid mitigates 3-Nitropropionic acid-induced Huntington’s disease via modulation of Nrf2/HO-1, TLR4/NF-κB, and SIRT1/p53 signaling pathways
synthesis and characterization of novel pyrazoline derivatives as dual α-amylase /α-glucosidase inhibitors: molecular modeling and kinetic study
Design and construction of novel pyridine-pyrimidine hybrids as selective COX-2 suppressors: anti-inflammatory potential, ulcerogenic profile, molecular modeling and ADME/Tox studies
Exploring Punicalagin Potential Against Cancers: A Comprehensive Review
Antioxidative and Anticancer Potential of Luteolin: A Comprehensive Approach Against Wide Range of Human Malignancies
In silico development of potential InhA inhibitors through 3D-QSAR analysis, virtual screening and molecular dynamics
Isatin derived morpholine and piperazine derivatives as acetylcholinesterase inhibitors
Recent Perspectives on Anticancer Potential of Coumarin Against Different Human Malignancies: An Updated Review
Biological activity and chemical characteristics studies of new oligomannose produced by Erwinia gerundensis
MAO-B Inhibitor (2E)-3-(4-Bromophenyl)-1-(1H-indol-3-yl) prop-2-en-1-one as a Neuroprotective Agent Against Alzheimer’s Disease
Inhibition of monoamine oxidases by heterocyclic derived conjugated dienones: synthesis and in vitro and in silico investigations
Discerning of isatin-based monoamine oxidase (MAO) inhibitors for neurodegenerative disorders by exploiting 2D, 3D-QSAR modelling and molecular dynamics simulation
α-Amylase enzyme inhibition relevant to type II diabetes by using functional yogurt with Cinnamomum verum and Stevia rebaudiana
Antioxidant, anticancer, and anti-inflammatory potential of Moringa seed and Moringa seed oil: A comprehensive approach
Impact of Some Natural and Artificial Sweeteners Consumption on Different Hormonal Levels and Inflammatory Cytokines in Male Rats: In Vivo and In Silico Studies
DOI: https://doi.org/10.1021/acsomega.4c01250?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
A literature review on pharmacological aspects, docking studies, and synthetic approaches of quinazoline and quinazolinone derivatives
Improving plant adaptation to soil antimony contamination: the synergistic contribution of arbuscular mycorrhizal fungus and olive mill waste
Chalcones with N‐Methylpiperazine Moiety: Synthesis, Monoamine Oxidase Inhibition, Neuroprotective Effect and Computer Simulation Study
Role of Probiotics against Human Cancers, Inflammatory Diseases, and Other Complex Malignancies
Machine learning driven web-based app platform for the discovery of monoamine oxidase B inhibitors
A structure-based approach to explore novel COX-2 inhibitors using pharmacophore modelling, 3D-QSAR analysis, virtual screening and dynamics simulation study
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
Polymeric Nanoparticles for Delivery of Natural Bioactive Agents: Recent Advances and Challenges
Urachal carcinoma: The journey so far and the road ahead
Phthalazone tethered 1,2,3-triazole conjugates: In silico molecular docking studies, synthesis, in vitro antiproliferative, and kinase inhibitory activities
Genetic Structure of Cucumber Mosaic Virus From Natural Hosts in Nigeria Reveals High Diversity and Occurrence of Putative Novel Recombinant Strains
Impact of Dietary Egg Yolk IgY Powder on Behavior, Meat Quality, Physiology, and Intestinal Escherichia coli Colonization of Broiler Chicks
Recommended and verified stability indicating GC–MS procedures for green separation of quaternary mixture of naphazoline, ephedrine, methylparaben, and naphazoline impurity
Royal Jelly and Chlorella vulgaris Mitigate Gibberellic Acid-Induced Cytogenotoxicity and Hepatotoxicity in Rats via Modulation of the PPARα/AP-1 Signaling Pathway and Suppression of Oxidative Stress and Inflammation
Berberine: a comprehensive Approach to combat human maladies
Targeting Some Key Metalloproteinases by Nano-Naringenin and Amphora coffeaeformis as a Novel Strategy for Treatment of Osteoarthritis in Rats
Development of Isopropyl-Tailed Chalcones as a New Class of Selective MAO-B Inhibitors for the Treatment of Parkinson’s Disorder
Phytochemical profile and pro-healthy properties of Terminalia chebula: A comprehensive review
Introduction of benzyloxy pharmacophore into aryl/ heteroaryl chalcone motifs as a new class of monoamine oxidase B inhibitors
Novel N-methylsulfonyl-indole derivatives: Biological activity and COX-2/5-LOX inhibitory effect with improved gastro protective profile and reduced cardio vascular risks
Two dimensional-QSAR and molecular dynamics studies of a selected class of aldoxime- and hydroxy-functionalized chalcones as monoamine oxidase-B inhibitors
Design, Synthesis, Molecular Modeling, and Anticancer Evaluation of New VEGFR-2 Inhibitors Based on the Indolin-2-One Scaffold
Chemical characteristics and targeted encapsulated Cordia myxa fruits extracts nanoparticles for antioxidant and cytotoxicity potentials
In Vitro Anti-Proliferative, and Kinase Inhibitory Activity of Phenanthroindolizidine Alkaloids Isolated from Tylophora indica
Morpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations
Novel Phenolic Compounds as Potential Dual EGFR and COX-2 Inhibitors: Design, Semisynthesis, in vitro Biological Evaluation and in silico Insights
Olive Oil/Pluronic Oleogels for Skin Delivery of Quercetin: In Vitro Characterization and Ex Vivo Skin Permeability
Trimethoxylated Halogenated Chalcones as Dual Inhibitors of MAO-B and BACE-1 for the Treatment of Neurodegenerative Disorders
Computational and Molecular Docking Studies of New Benzene Sulfonamide Drugs with Anticancer and Antioxidant Effects
Development and assessment of phospholipid-based luteolin-loaded lipid nanocapsules for skin delivery
Efects of radiation exposure on brain health: a state of the art and new challenges
Nanoparticle-based therapeutic approaches for wound healing: a review of the state-of-the-art
Chitosan-Functionalized-Graphene Oxide (GO@CS) Beads as an Effective Adsorbent to Remove Cationic Dye from Wastewater
High-Pressure Metal-Free Catalyzed One-Pot Two-Component Synthetic Approach for New 5-Arylazopyrazolo[3,4-b]Pyridine Derivatives
Development of Halogenated-Chalcones Bearing with Dimethoxy Phenyl Head as Monoamine Oxidase-B Inhibitors
New Sulfamethoxazole Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors: Design, Synthesis, Cytotoxic Activity and Molecular Modeling
Preventive Effects of Mandarin Fruit Peel Hydroethanolic Extract, Hesperidin, and Quercetin on Acetaminophen-Induced Hepatonephrotoxicity in Wistar Rats
Nanocomposite of gold nanoparticles@nickel disulfide-plant derived carbon for molecularly imprinted electrochemical determination of favipiravir
Bilosomes as a promising nanoplatform for oral delivery of an alkaloid nutraceutical: improved pharmacokinetic profile and snowballed hypoglycemic effect in diabetic rats
LC/MS Profiling and Gold Nanoparticle Formulation of Major Metabolites from Origanum majorana as Antibacterial and Antioxidant Potentialities
Development of a Novel Class of Pyridazinone Derivatives as Selective MAO-B Inhibitors
Azides in the Synthesis of Various Heterocycles
Development of bromo- and fluoro-based α, β-unsaturated ketones as highly potent MAO-B inhibitors for the treatment of Parkinson’s disease
Design, Synthesis and Anticancer Profile of New 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-Linked Sulfonamide Derivatives with V600EBRAF Inhibitory Effect
Emerging Anthelmintic Resistance in Poultry: Can Ethnopharmacological Approaches Offer a Solution
On dynamics of an eco-epidemics system incorporating fractional operators of singular and nonsingular types
A new green approach for the reduction of consumed solvents and simultaneous quality control analysis of several pharmaceuticals using a fast and economic RP-HPLC method; a case study for a mixture of piracetam, ketoprofen and omeprazole drugs
Optimization of pyrazolo[1,5-a]pyrimidine based compounds with pyridine scaffold: Synthesis, biological evaluation and molecular modeling study
Triazoloquinoxalines-based DNA intercalators-Topo II inhibitors: design, synthesis, docking, ADMET and anti-proliferative evaluations
Efficiency of Multiple Extraction Solvents on Antioxidant, Cytotoxic, and Phytotoxic Potential of Taraxacum officinale (L.) Weber ex F.H. Wigg. from Poonch Valley, Azad Kashmir, Pakistan
Chitosan Silver and Gold Nanoparticle Formation Using Endophytic Fungi as Powerful Antimicrobial and Anti-Biofilm Potentialities
The nutraceutical properties and health benefits of pseudocereals: a comprehensive treatise
Exploration of the Detailed Structure–Activity Relationships of Isatin and Their Isomers As Monoamine Oxidase Inhibitors
Investigation of Chemical Compositions and Biological Activities of Mentha suaveolens L. from Saudi Arabia
Novel Pyridinium Based Ionic Liquid Promoter for Aqueous Knoevenagel Condensation: Green and Efficient Synthesis of New Derivatives with Their Anticancer Evaluation
Knowledge, Attitudes and Practices of Pharmacogenomics Among Senior Pharmacy Students: A Cross Sectional Study from Punjab, Pakistan
A meta-analysis showing the effect of surgical site wound infections and associated risk factors in neonatal surgeries
Review of the Recent Advances in Electrospun Nanofibers Applications in Water Purification
Antibacterial and Wound-Healing Activities of Statistically Optimized Nitrofurazone- and Lidocaine-Loaded Silica Microspheres by the Box–Behnken Design
Recent Progress and Potential Biomedical Applications of Electrospun Nanofibers in Regeneration of Tissues and Organs
Biological investigation of N-methyl thiosemicarbazones as antimicrobial agents and bacterial carbonic anhydrases inhibitors
Cubosomes as an emerging platform for drug delivery: a state-of-the-art review
Design, synthesis, and biological evaluation of novel pyrido-dipyrimidines as dual topoisomerase II/FLT3 inhibitors in leukemia cells
Pioglitazone Synthetic Analogue Ameliorates Streptozotocin-Induced Diabetes Mellitus through Modulation of ACE 2/Angiotensin 1–7 via PI3K/AKT/mTOR Signaling Pathway
The Chemical Profiling, Docking Study, and Antimicrobial and Antibiofilm Activities of the Endophytic fungi Aspergillus sp. AP5
Assessment of Nasal-Brain-Targeting Efficiency of New Developed Mucoadhesive Emulsomes Encapsulating an Anti-Migraine Drug for Effective Treatment of One of the Major Psychiatric Disorders Symptoms
Design, Molecular Docking, Synthesis, Anticancer and Anti-Hyperglycemic Assessments of Thiazolidine-2,4-Diones Bearing Sulfonylthiourea Moieties as Potent VEGFR-2 Inhibitors and PPARγ Agonists
Conjugated Dienones from Differently Substituted Cinnamaldehyde as Highly Potent Monoamine Oxidase?B Inhibitors: Synthesis, Biochemistry, and Computational Chemistry
DOI: https://doi.org/10.1021/acsomega.2c00397?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
EGFR and COX-2 Dual Inhibitor: The Design, Synthesis, and Biological Evaluation of Novel Chalcones
Targeting tumor cells with pyrazolo[3,4-d] pyrimidine scaffold: A literature review on synthetic approaches, structure activity relationship, structural and target-based mechanisms
Docking Study, Synthesis, and Anti-Inflammatory Potential of Some New Pyridopyrimidine-Derived Compounds
Development and Greenness Assessment of HPLC Method for Studying the Pharmacokinetics of Co-Administered Metformin and Papaya Extract
Article Solulan C24- and Bile Salts-Modified Niosomes for New Ciprofloxacin Mannich Base for Combatting Pseudomonas-Infected Corneal Ulcer in Rabbits
Solulan C24- and Bile Salts-Modified Niosomes for New Ciprofloxacin Mannich Base for Combatting Pseudomonas-Infected Corneal Ulcer in Rabbits
Identifcation of non‑classical hCA XII inhibitors using combination of computational approaches for drug design and discovery
Evaluation of Ligustrazine-Based Synthetic Compounds for their Antiproliferative Effects
Replacement of Chalcone-Ethers with Chalcone-Thioethers as Potent and Highly Selective Monoamine Oxidase-B Inhibitors and Their Protein-Ligand Interactions
Synthesis of New 1-Aryl-2-(3,5-dimethylpyrazol-1-yl)ethanone Oxime Ether Derivatives and Investigation of Their Cytotoxic Effects
Evaluation of ligustrazine based synthetic compounds for mechanism based antiproliferative effects
Revealing the role of fluorine pharmacophore in chalcone scaffold for shifting the MAO-B selectivity: investigation of a detailed molecular dynamics and quantum chemical study
Halogenated Coumarin?Chalcones as Multifunctional Monoamine Oxidase?B and Butyrylcholinesterase Inhibitors
DOI: https://doi.org/10.1021/acsomega.1c04252?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
Halogenated Coumarin−Chalcones as Multifunctional Monoamine Oxidase‑B and Butyrylcholinesterase Inhibitors
DOI: https://doi.org/10.1021/acsomega.1c04252?urlappend=%3Fref%3DPDF&jav=VoR&rel=cite-as
Selected Class of Enamides Bearing Nitro Functionality as Dual-Acting with Highly Selective Monoamine Oxidase-B and BACE1 Inhibitors
Design, Synthesis and Anticancer Profile of New 4-(1H-benzo[d]imidazol-1-yl)pyrimidin-2-amine-Linked Sulfonamide Derivatives with V600EBRAF Inhibitory Effect
Navigating into the Chemical Space of Monoamine Oxidase Inhibitors by Artificial Intelligence and Cheminformatics Approach
Strawberry and Ginger Silver Nanoparticles as Potential Inhibitors for SARS-CoV-2 Assisted by In Silico Modeling and Metabolic Profiling
Identification of non-classical hCA XII inhibitors using combination of computational approaches for drug design and discovery
Synthesis of N0 -(4-/3-/2-/Non-substituted benzylidene)- 4-[(4-methylphenyl)sulfonyloxy] Benzohydrazides and Evaluation of Their Inhibitory Activities against Monoamine Oxidases and β-Secretase
Synthesis of N′-(4-/3-/2-/Non-substituted benzylidene)-4-[(4-methylphenyl)sulfonyloxy] Benzohydrazides and Evaluation of Their Inhibitory Activities against Monoamine Oxidases and β-Secretase
Trimethoxylated Halogenated Chalcones as Dual Inhibitors of MAO-B and BACE-1 for the Treatment of Neurodegenerative Disorders
Trimethoxylated Halogenated Chalcones as Dual Inhibitors of MAO-B and BACE-1 for the Treatment of Neurodegenerative Disorders
Development of Halogenated Pyrazolines as Selective Monoamine Oxidase-B Inhibitors: Deciphering via Molecular Dynamics Approach
Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells
Cytotoxic Potential, Metabolic Profiling, and Liposomes of Coscinoderma sp. Crude Extract Supported by in silico Analysis
Simultaneous analysis of several antihypertensive drugs in different combinations: Application for determination of drug degradation products and process impurities
Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities
New Benzoxazole Derivatives as Antiprotozoal Agents: In Silico Studies, Synthesis, and Biological Evaluation
A New CDK2 Inhibitor with 3-Hydrazonoindolin-2-One Scaffold Endowed with Anti-Breast Cancer Activity: Design, Synthesis, Biological Evaluation, and In Silico Insights