Diarylheterocycle Core Ring Features Effect in Selective COX‐1 Inhibition

No abstract is available for this paper.

• Publication year

  2012

• Venue

  ChemMedChem

• Publication date

  2012-04-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1002/cmdc.201100530PMID 22278975
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Novel selective COX-1 inhibitors suppress neuroinflammatory mediators in LPS-stimulated N13 microglial cells.

  2012cited by this paper
• Pharmacological profile of FK881(ASP6537), a novel potent and selective cyclooxygenase-1 inhibitor.

  2011cited by this paper
• A nimesulide derivative with potential anti-inflammatory activity: Synthesis, X-ray powder structure analysis and DFT study

  2010cited by this paper
• Molecular Basis for Cyclooxygenase Inhibition by the Non-steroidal Anti-inflammatory Drug Naproxen*

  2010cited by this paper
• Molecular basis of cyclooxygenase enzymes (COXs) selective inhibition

  2010cited by this paper
• Selective COX-1 inhibition: A therapeutic target to be reconsidered.

  2010cited by this paper
• Structural Basis of Fatty Acid Substrate Binding to Cyclooxygenase-2*

  2010cited by this paper
• EXPO2009: structure solution by powder data in direct and reciprocal space

  2009cited by this paper
• Advances in powder diffraction pattern indexing: N-TREOR09

  2009cited by this paper
• Coxibs interfere with the action of aspirin by binding tightly to one monomer of cyclooxygenase-1

  2009cited by this paper
• Improved regioselectivity in pyrazole formation through the use of fluorinated alcohols as solvents: synthesis and biological activity of fluorinated tebufenpyrad analogs.

  2008cited by this paper
• Effect of the aryl group substituent in the dimerization of 3-arylisoxazoles to syn 2,6-diaryl-3,7-diazatricyclo[4.2.0.02,5]octan-4,8-diones induced by LDA

  2008cited by this paper
• Correcting resolution bias in electron density maps of organic molecules derived by direct methods from powder data

  2008cited by this paper
• Straightforward transformation of isoxazoles into pyrazoles: renewed and improved

  2007cited by this paper
• Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.

  2005cited by this paper
• 5-Hydroxy-3-phenyl-5-vinyl-2-isoxazoline and 3-phenyl-5-vinylisoxazole: synthesis and reactivity

  2005cited by this paper
• Reaction of 3-phenylisoxazole with alkyllithiums

  2005cited by this paper
• Haloacetylated Enol Ethers, 19: Synthesis of 3-(2-Thienyl)- and 3-(2-Furyl)-5-trihalomethyl Substituted Azoles

  2005cited by this paper
• UCSF Chimera—A visualization system for exploratory research and analysis

  2004cited by this paper
• Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal.

  2004cited by this paper
• Crystal Structure of Arachidonic Acid Bound to a Mutant of Prostaglandin Endoperoxide H Synthase-1 That Forms Predominantly 11-Hydroperoxyeicosatetraenoic Acid*

  2004cited by this paper
• The 2.0 A resolution crystal structure of prostaglandin H2 synthase-1: structural insights into an unusual peroxidase.

  2004cited by this paper
• Structural approach for COX-2 inhibition.

  2004cited by this paper
• Organic Fluorine: Odd Man Out

  2004cited by this paper
• Improved protein–ligand docking using GOLD

  2003cited by this paper
• Synthesis of fluorinated heterocycles

  2002cited by this paper
• Mechanism of inhibition of novel COX-2 inhibitors.

  2002cited by this paper
• The PyMOL Molecular Graphics System

  2002cited by this paper
• Regioselective synthesis and side-chain metallation and elaboration of 3-aryl-5-alkylisoxazoles

  2002cited by this paper
• Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility.

  2001cited by this paper
• Mutational and X-ray Crystallographic Analysis of the Interaction of Dihomo-γ-linolenic Acid with Prostaglandin Endoperoxide H Synthases*

  2001cited by this paper
• Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.

  2000cited by this paper
• The productive conformation of arachidonic acid bound to prostaglandin synthase.

  2000cited by this paper
• The penultimate rotamer library

  2000cited by this paper
• The Dynamics of Prostaglandin H Synthases

  1998cited by this paper
• Pharmacological analysis of cyclooxygenase-1 in inflammation.

  1998cited by this paper
• Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).

  1997cited by this paper
• Organic Fluorine Hardly Ever Accepts Hydrogen Bonds

  1997cited by this paper
• Empirical scoring functions: I. The development of a fast empirical scoring function to estimate the binding affinity of ligands in receptor complexes

  1997cited by this paper
• Development and validation of a genetic algorithm for flexible docking.

  1997cited by this paper
• Differential Utilization of Trk Autophosphorylation Sites*

  1996cited by this paper
• Flexibility of the NSAID binding site in the structure of human cyclooxygenase-2

  1996cited by this paper
• Involvement of Arginine 120, Glutamate 524, and Tyrosine 355 in the Binding of Arachidonate and 2-Phenylpropionic Acid Inhibitors to the Cyclooxygenase Active Site of Ovine Prostaglandin Endoperoxide H Synthase-1 (*)

  1996cited by this paper
• Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents

  1996cited by this paper
• Antiplatelet agents based on cyclooxygenase inhibition without ulcerogenesis. Evaluation and synthesis of 4,5-bis(4-methoxyphenyl)-2-substituted-thiazoles.

  1994cited by this paper
• The X-ray crystal structure of the membrane protein prostaglandin H2 synthase-1

  1994cited by this paper
• Ab-initio structure determination of LiSbWO6 by X-ray powder diffraction

  1988cited by this paper
• Pyrrole and Pyrazole Ring Closure in Heterogeneous Media

  1986cited by this paper
• Profile shape functions in Rietveld refinements

  1982cited by this paper
• A profile refinement method for nuclear and magnetic structures

  1969cited by this paper
• Synthesis of isothiazoles

  1969cited by this paper
• A simplified criterion for the reliability of a powder pattern indexing

  1968cited by this paper

• Assembly of CF3-Pyrazole-Triazole Hybrids through (3 + 3)-Cycloaddition/Ring Contraction and Click Chemistry.

  2026cites this paper
• Therapeutic Role of Cyclooxygenase-1 (COX-1) Inhibition, Challenging the Conventional View of COX-1 as Purely Constitutive.

  2026cites this paper
• Synthesis, molecular dynamics simulation, and evaluation of biological activity of novel flurbiprofen and ibuprofen‐like compounds

  2024cites this paper
• Synthesis, Docking, and DFT Studies on Novel Schiff Base Sulfonamide Analogues as Selective COX-1 Inhibitors with Anti-Platelet Aggregation Activity

  2024influential citation
• Phosphorylated 5-tert-Butyl-2 and 3-Furylalkenes: Synthesis and Heterocyclization

  2024cites this paper
• Trifluoromethyl-β-dicarbonyls as Versatile Synthons in Synthesis of Heterocycles.

  2023cites this paper
• Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.

  2021cites this paper
• Sequential [3+2] annulation reaction of prop-2-ynylsulfonium salts and hydrazonyl chlorides: synthesis of pyrazoles containing functional motifs.

  2021cites this paper
• Synthesis, Biological Activity, and Molecular Modeling Studies of Pyrazole and Triazole Derivatives as Selective COX-2 Inhibitors

  2020cites this paper
• Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.

  2019cites this paper
• A chemo- and regiocontrolled approach to bipyrazoles and pyridones via the reaction of ethyl 5-acyl-4-pyrone-2-carboxylates with hydrazines.

  2018cites this paper
• New 1,3,4-oxadiazole/oxime hybrids: Design, synthesis, anti-inflammatory, COX inhibitory activities and ulcerogenic liability.

  2017cites this paper
• Novel quinoline incorporating 1,2,4-triazole/oxime hybrids: Synthesis, molecular docking, anti-inflammatory, COX inhibition, ulceroginicity and histopathological investigations.

  2017cites this paper
• Phytochemical Characterization and Biological Evaluation of the Aqueous and Supercritical Fluid Extracts from Salvia sclareoides Brot

  2017cites this paper
• New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.

  2017cites this paper
• Isoxazole‐Based‐Scaffold Inhibitors Targeting Cyclooxygenases (COXs)

  2016cites this paper
• Novel 1,3,4-oxadiazole/oxime hybrids: Synthesis, docking studies and investigation of anti-inflammatory, ulcerogenic liability and analgesic activities.

  2016cites this paper
• COX‐1 Inhibitors: Beyond Structure Toward Therapy

  2016cites this paper
• The antiproliferative and proapoptotic effects of cladosporols A and B are related to their different binding mode as PPARγ ligands.

  2016cites this paper
• General role of the amino and methylsulfamoyl groups in selective cyclooxygenase(COX)-1 inhibition by 1,4-diaryl-1,2,3-triazoles and validation of a predictive pharmacometric PLS model.

  2015cites this paper
• Update on SAR Studies Toward New COX-1 Selective Inhibitors.

  2015cites this paper
• COX inhibitors: a patent review (2011 – 2014)

  2015cites this paper
• Crystal structures of two 6-(2-hydroxybenzoyl)-5H-thiazolo[3,2-a]pyrimidin-5-ones

  2015cites this paper
• Coumarins as privileged scaffold for anti-inflammatory drug development

  2015cites this paper
• Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles.

  2014cites this paper
• From 4,5,6,7-tetrahydroindoles to 3- or 5-(4,5,6,7-tetrahydroindol-2-yl)isoxazoles in two steps: a regioselective switch between 3- and 5-isomers

  2014cites this paper
• Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.

  2014cites this paper
• PET radiotracer [¹⁸F]-P6 selectively targeting COX-1 as a novel biomarker in ovarian cancer: preliminary investigation.

  2014cites this paper
• Novel 1-[4-(Aminosulfonyl)phenyl]-1H-1,2,4-triazole derivatives with remarkable selective COX-2 inhibition: design, synthesis, molecular docking, anti-inflammatory and ulcerogenicity studies.

  2014cites this paper
• Identification of a new series of amides as non-covalent proteasome inhibitors.

  2014cites this paper
• Exploring the reactivity of dimethylzinc with fluorine substituted 1-phenyl-4,5-dihydro-1H-pyrazol-5-ols

  2014cites this paper
• Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3-c]pyrazol-4(1H)-ones as potential cyclooxygenase-2 (COX-2) inhibitors.

  2014cites this paper
• Development of Novel Selective Peptidomimetics Containing a Boronic Acid Moiety, Targeting the 20S Proteasome as Anticancer Agents

  2014cites this paper
• Development of peptidomimetic boronates as proteasome inhibitors.

  2013cites this paper
• Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors.

  2013cites this paper
• Five-membered Ring Heterocycles by Reacting Enolates with Dipoles

  2013cites this paper
• Design, synthesis and molecular docking study of some substituted 4,5- dihydro-2H-indazole derivatives as potential anti-inflammatory agents.

  2013cites this paper