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Pubblicazioni
JOURNAL OF MEDICINAL CHEMISTRY
Rivista
Codice:
E092714
ISSN:
0022-2623
Dati Generali
Dati Generali
Pubblicazioni (102)
Pulisci
Ordina Pubblicazioni:
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decrescente
1 '-Benzyl-3,4-dihydrospiro[2H-1-benzothiopyran-2,4 '-piperidine] (Spipethiane), a potent and highly selective sigma(1) ligand
Articolo
1,3-Dioxolane-Based Ligands as a Novel Class of Alpha1-Adrenoceptor Antagonists
Articolo
1-Benzopyran-4-one antioxidants as aldose reductase inhibitors
Articolo
2-(2-phenylcyclopropyl) imidazolines: Reversed enantioselective interaction at I-1 and I-2 imidazoline receptors
Articolo
2-{[(2-(2,6-Dimethoxyphenoxy)ethyl]}-1,4-benzoxathiano:A New Antagonist With High Potency and Selectivity Toward alpha1-Adrenoreceptors.
Articolo
2′-Deoxyuridine 5′-Monophosphate Substrate Displacement in Thymidylate Synthase through 6-Hydroxy-2H-naphtho[1,8-bc]furan-2-one Derivatives
Articolo
A Common Mechanism Underlying Promiscuous Inhibitors from Virtual and High-Throughput Screening
Articolo
Adenosine A(2A) Receptor-Antagonist/Dopamine D(2) Receptor-Agonist Bivalent Ligands as Pharmacological Tools to Detect A(2A)-D(2) Receptor Heteromers
Articolo
Alanine Mutants of the Interface Residues of Human Thymidylate Synthase Decode Key Features of the Binding Mode of Allosteric Anticancer Peptides
Articolo
Alpha2-Adrenoceptors Profile Modulation anf High Antinociceptove Activity of (S)-)2-[1-(Biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole
Articolo
Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships
Articolo
Antibacterial agent discovery using thymidylate synthase biolibrary screening
Articolo
Antitarget, Anti-SARS-CoV-2 Leads, Drugs, and the Drug Discovery-Genetics Alliance Perspective
Articolo
BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring
Articolo
Characterization of 2,4-Diamino-6-oxo-1,6-dihydropyrimidin-5-yl Ureido Based Inhibitors of Trypanosoma brucei FolD and Testing for Antiparasitic Activity
Articolo
Click Chemistry in Lead Optimization of Boronic Acids as β-Lactamase Inhibitors
Articolo
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against β-lactamase
Articolo
Conformational Propensity and Biological Studies of Proline Mutated LR Peptides Inhibiting Human Thymidylate Synthase and Ovarian Cancer Cell Growth
Articolo
Corrections to pyridoimidazolones as novel potent inhibitors of v-raf murine sarcoma viral oncogene homologue B1 (BRAF) (Journal of Medicinal Chemistry (2009) 52, (2255-2256) DOI: 10.1021/jm801509w)
Articolo
Design and exploration of novel boronic acid Inhibitors reveals important Interactions with a clavulanic acid-resistant sulfhydryl- variable (SHV) β‑ lactamase
Articolo
Design, Synthesis, Strucural Studies, Biological Evaluation, and Computational Simulations of Novel Potent AT1 Angiotensin II Receptor Antagonists Based on the 4-Phenylquinoline Structure
Articolo
Design, synthesis, and physicochemical and biological characterization of a new iron chelator of the family of hydroxychromenes
Articolo
Design, synthesis, crystal structures and antimicrobial activity of sulfonamide boronic acids as beta-lactamase inhibitors
Articolo
Designing Chimeric Molecules for Drug Discovery by Leveraging Chemical Biology
Articolo
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): Increasing cellular potency through optimization of a distal heteroaromatic group
Articolo
Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases
Articolo
Docking and database screening reveal new classes of Plasmodium falciparum dihydrofolate reductase inhibitors
Articolo
Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective
Articolo
Enantioselectivity of Muscarinic Antagonists. 2,2-Dicyclohexyl-5-((dimethylamino)methyl)-1,3-oxathiolane Methiodide and Related 3-oxide.
Articolo
Enantioselectivity of Muscarinic Antagonists. Isomeric 2-Cyclohexyl-2-phenyl-5-(dimethylamino)methyl)-1,3-oxathiolane
Articolo
Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections
Articolo
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5
Articolo
Exploring Translocator Protein (TSPO) Medicinal Chemistry: An Approach for Targeting Radionuclides and Boron Atoms to Mitochondria
Articolo
Folic Acid-Peptide Conjugates Combine Selective Cancer Cell Internalization with Thymidylate Synthase Dimer Interface Targeting
Articolo
Further studies on the interaction of the 5-hydroxytryptamine(3) (5-HT3) receptor with arylpiperazine ligands. Development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties
Articolo
High-Throughput Phenotypic Screening and Machine Learning Methods Enabled the Selection of Broad-Spectrum Low-Toxicity Antitrypanosomatidic Agents
Articolo
Hotspots in an obligate homodimeric anticancer target. structural and functional effects of interfacial mutations in human thymidylate synthase
Articolo
Imidazoline binding sites (IBS) profile modulation: Key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues
Articolo
Immunostimulation by a partially retro-inverso tuftsin analogue containing Thr 1 (NHCO) (R,S) Lys 2 modification
Articolo
Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine
Articolo
Inhibitor of Ovarian Cancer Cells growth by Virtual Screening: A New Thiazole Derivative Targeting Human Thymidylate Synthase
Articolo
Internalization and stability of a thymidylate synthase peptide inhibitor in ovarian cancer cells
Articolo
Isoxazolo-[3,4-d]-pyridazin-7-(6H)-one as a potential substrate for new aldose reductase inhibitors
Articolo
Mapping and fitting the peripheral benzodiazepine receptor binding site by carboxamide derivatives. Comparison of different approaches to quantitative ligand-receptor interaction modeling
Articolo
Mapping the peripheral benzodiazepine receptor binding site by conformationally restrained derivatives of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide (PK11195)
Articolo
Mono- and Disubstituted-3,8-diazabicyclo[3.2.1]octane Derivatives as Analgesics Structurally Related to Epibatidine: Synthesis, Activity, and Modeling.
Articolo
Multitarget, Selective Compound Design Yields Potent Inhibitors of a Kinetoplastid Pteridine Reductase 1
Articolo
Negative Allosteric Modulators of A2AR: A New Weapon for Cancer Immunotherapy?
Articolo
New Improved cGMP Analogues to Target Rod Photoreceptor Degeneration
Articolo
Newly synthesized curcumin derivatives: crosstalk between chemico-physical properties and biological activity.
Articolo
Non-peptide ligands for opioid receptors. Design of k-specific agonists
Articolo
Novel Approaches for Targeting Thymidylate Synthase to Overcome the Resistance and Toxicity of Anticancer Drugs
Articolo
Novel Potent BRAF Inhibitors: Toward 1 nM Compounds through Optimization of the Central Phenyl Ring
Articolo
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors
Articolo
Novel potent AMPA/kainate receptor antagonists: Synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4, 5-methylenedioxyphenylacetic Acid alkyl esters
Articolo
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives
Articolo
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors
Articolo
Optimization of Peptides That Target Human Thymidylate Synthase to Inhibit Ovarian Cancer Cell Growth
Articolo
Optimizing Cell Permeation of an Antibiotic Resistance Inhibitor for Improved Efficacy
Articolo
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists
Articolo
Phthalein derivatives as a new tool for selectivity in thymidylate synthase inhibition
Articolo
Polypharmacology: challenges and opportunities in drug discovery
Articolo
Profiling of Flavonol Derivatives for the Development of Antitrypanosomatidic Drugs
Articolo
Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF)
Articolo
Quantitative Structure-Activity Analysis in Dihydropteroate Synthase Inhibition by Sulphones. Comparison with Sulfanilamides.
Articolo
Quantitative Structure-Activity Relationships in Dihydropteroate Synthase Inhibition by Multisubstituted Sulfones. Design and Synthesis of Some New Derivatives with Improved Potency.
Articolo
Resolution, Absolute Configuration and Cholinergic Enantioselectivity of (+) and (-) cis-2-Methyl-5-dimethylaminomethyl-1,3-oxathiolane Methiodide.
Articolo
Resolution, Absolute Configuration and Cholinergic Enantioselectivity of (-) and (+) c-2-Methyl-r-5-((Dimethylamino(methyl)-1,3-oxathiuolane-t-oxide Methiodide and Related Sulfones.
Articolo
Soft docking and multiple receptor conformations in virtual screening.
Articolo
Structure-Activity Relationship in Dihydropteroate Synthase Inhibition by Sulfanilamides. Comparison with the Antibacterial Activity.
Articolo
Structure-Activity Relationships Among Benextramine Related Tetramine Disulfidxe. Chain Length Effect on alpha-adrenoreceptor Blocking Activity.
Articolo
Structure-Activity Relationships Among Benextramine-Related Tetramine Disulfide at Peripheral Alpha-Adrenoreceptors.
Articolo
Structure-Activity Relationships for Prazosin and WB4101 Analogues as alpha1-Adrenoreceptor Antagonist.
Articolo
Structure-Activity Relationships in 1,4-Benzodioxane Related Compounds. Investigation on the Role of the Dehydrodioxane Ring on alpha1-Adrenoreceptor Blocking Activity.
Articolo
Structure-Activity Relationships in Prazosin-Related Compounds. Effect of Replacing a Piuperazine Ring with an Alkanediamine Moiety on alpa1-Adrenoreceptor Blocking Activity.
Articolo
Structure-Based Design of Potent Aromatase Inhibitors by High-Throughput Docking
Articolo
Structure-Based Discovery of Hsp90/HDAC6 Dual Inhibitors Targeting Aggressive Prostate Cancer
Articolo
Structure-Based Selectivity Optimization of Piperidine–Pteridine Derivatives as Potent Leishmania Pteridine Reductase Inhibitors
Articolo
Structure_Activity Relationships among Methoctramine-Related Polymethylene Tetramine. Chain Length and Substituent Effects on M2 Muscarinic Receptor Blocking Activity.
Articolo
Synthesis and anticonvulsant activity of novel and potent 2,3- benzodiazepine AMPA/kainate receptor antagonists
Articolo
Synthesis and anticonvulsant activity of novel and potent 6,7- methylenedioxyphthalazin-1(2H)-ones
Articolo
Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase
Articolo
Synthesis and evaluation of antiparasitic activities of new 4-[5-(4-phenoxyphenyl)-2H-pyrazol-3-yl]morpholine derivatives
Articolo
Synthesis and structure-activity relationships of 1-aralkyl-4- benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent σ ligands
Articolo
Synthesis of 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide derivatives as potential allosteric modulators of AMPA/Kainate receptors
Articolo
Synthesis of a Novel Boronic Acid Transition State Inhibitor, MB076: A Heterocyclic Triazole Effectively Inhibits Acinetobacter-Derived Cephalosporinase Variants with an Expanded-Substrate Spectrum
Articolo
Synthesis, activity, and molecular modeling of a new series of tricyclic pyridazinones as selective aldose reductase inhibitors
Articolo
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors
Articolo
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity
Articolo
Synthesis, pharmacological evaluation, and structure-activity relationship and quantitative structure-activity relationship studies on novel derivatives of 2,4-diamino-6,7-dimethoxyquinazoline alpha(1)-adrenoceptor antagonists
Articolo
Synthesis, resolution, and preliminary evaluation of trans-2-amino-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes and related derivatives as dopamine receptors ligands
Articolo
Synthesis, screening, and molecular modeling of new potent and selective antagonists at the alpha(1d) adrenergic receptor
Articolo
Target Flexibility: An Emerging Consideration in Drug Discovery and Design
Articolo
Targeting Class A and C Serine β-Lactamases with a Broad-Spectrum Boronic Acid Derivative
Articolo
Ten years of medicinal chemistry (2005-2014) in the journal of medicinal chemistry: Country of contributors, topics, and public-private partnerships miniperspective
Articolo
The Hippo Pathway and YAP/TAZ-TEAD Protein-Protein Interaction as Targets for Regenerative Medicine and Cancer Treatment
Articolo
The binding of benzenesulfonamides to carbonic anhydrase enzyme. A molecular mechanics study and quantitative structure-activity relationships
Articolo
Three-dimensional quantitative structure-activity relationship analysis of a set of Plasmodium falciparum dihydrofolate reductase inhibitors using a pharmacophore generation approach
Articolo
Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-1-(2′, 4′-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7] cyclohepta[1,2-c]pyrazole-3-carboxamide
Articolo
Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB 2 cannabinoid ligand 1-(2′, 4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c] pyrazole-3-carboxamide
Articolo
Virtual Screening and X-ray Crystallography Identify Non-Substrate Analog Inhibitors of Flavin-Dependent Thymidylate Synthase
Articolo
Virtual screening identification of nonfolate compounds, including a CNS drug, as antiparasitic agents inhibiting pteridine reductase
Articolo
No Results Found
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