84 articles for thisTarget
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New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
University of Bari Aldo Moro
Quinolino[3,4-b]quinoxalines and pyridazino[4,3-c]quinoline derivatives: Synthesis, inhibition of topoisomerase IIa, G-quadruplex binding and cytotoxic properties.
University of Bari Aldo Moro
Structural modifications of the serotonin 5-HT7 receptor agonist N-(4-cyanophenylmethyl)-4-(2-biphenyl)-1-piperazinehexanamide (LP-211) to improve in vitro microsomal stability: A case study.
University of Bari Aldo Moro
The chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca(2+)/calmodulin-dependent kinase II.
University of Bari Aldo Moro
Development of sigma-1 (s1) receptor fluorescent ligands as versatile tools to studys1 receptors.
University of Bari Aldo Moro
Novel 3-(1H-indol-3-yl)-2-[3-(4-methoxyphenyl)ureido]propanamides as selective agonists of human formyl-peptide receptor 2.
University of Bari Aldo Moro
Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases.
University of Bari Aldo Moro
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.
University of Bari Aldo Moro
Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptora/¿ ligand LT175.
University of Bari Aldo Moro
Trimethoxybenzanilide-based P-glycoprotein modulators: an interesting case of lipophilicity tuning by intramolecular hydrogen bonding.
University of Bari Aldo Moro
Deconstruction of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline moiety to separate P-glycoprotein (P-gp) activity froms2 receptor affinity in mixed P-gp/s2 receptor agents.
University of Bari Aldo Moro
From mixed sigma-2 receptor/P-glycoprotein targeting agents to selective P-glycoprotein modulators: small structural changes address the mechanism of interaction at the efflux pump.
University of Bari Aldo Moro
Discovery of new 7-substituted-4-imidazolylmethyl coumarins and 4'-substituted-2-imidazolyl acetophenones open analogues as potent and selective inhibitors of steroid-11ß-hydroxylase.
University of Bari Aldo Moro
In silico design of novel 2H-chromen-2-one derivatives as potent and selective MAO-B inhibitors.
University of Bari Aldo Moro
SAR studies on tetrahydroisoquinoline derivatives: the role of flexibility and bioisosterism to raise potency and selectivity toward P-glycoprotein.
University of Bari Aldo Moro
Synthesis, Characterization, and in Vitro Evaluation of a New TSPO-Selective Bifunctional Chelate Ligand.
University of Bari Aldo Moro
Dual carbonic anhydrase/matrix metalloproteinase inhibitors incorporating bisphosphonic acid moieties targeting bone tumors.
University of Bari Aldo Moro
Novel derivatives of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) with improved fluorescent ands receptors binding properties.
University of Bari Aldo Moro
Arylamino bisphosphonates: potent and selective inhibitors of the tumor-associated carbonic anhydrase XII.
University of Bari Aldo Moro
Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.
University of Bari Aldo Moro
Arylamino methylene bisphosphonate derivatives as bone seeking matrix metalloproteinase inhibitors.
University of Bari Aldo Moro
Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging ofs2 receptors.
University of Bari Aldo Moro
Activity-lipophilicity relationship studies on P-gp ligands designed as simplified tariquidar bulky fragments.
University of Bari Aldo Moro
Investigation ofs receptors agonist/antagonist activity through N-(6-methoxytetralin-1-yl)- and N-(6-methoxynaphthalen-1-yl)alkyl derivatives of polymethylpiperidines.
University of Bari Aldo Moro
Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp.
University of Bari Aldo Moro
Naphthalenyl derivatives for hitting P-gp/MRP1/BCRP transporters.
University of Bari Aldo Moro
Discovery, biological evaluation, and structure-activity and -selectivity relationships of 6'-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-methylacetamides, a novel class of potent and selective monoamine oxidase inhibitors.
University of Bari Aldo Moro
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.
University of Bari Aldo Moro
Structural insights into monoamine oxidase inhibitory potency and selectivity of 7-substituted coumarins from ligand- and target-based approaches.
University of Bari Aldo Moro
Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novela1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, anda1d computational study.
University of Bari Aldo Moro
Design, synthesis, and pharmacological effects of structurally simple ligands for MT(1) and MT(2) melatonin receptors.
University of Bari Aldo Moro
2D- and 3D-QSAR of tocainide and mexiletine analogues acting as Na(v)1.4 channel blockers.
University of Bari Aldo Moro
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.
University of Bari Aldo Moro
Novel 2-phenylimidazo[1,2-a]pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity, and in vivo studies.
University of Bari Aldo Moro
Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.
University of Bari Aldo Moro
Design, synthesis and biological evaluation of 5-hydroxy, 5-substituted-pyrimidine-2,4,6-triones as potent inhibitors of gelatinases MMP-2 and MMP-9.
University of Bari Aldo Moro
Design, synthesis and biological evaluation of benzo[e][1,2,4]triazin-7(1H)-one and [1,2,4]-triazino[5,6,1-jk]carbazol-6-one derivatives as dual inhibitors of beta-amyloid aggregation and acetyl/butyryl cholinesterase.
University of Bari Aldo Moro
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
University of Bari Aldo Moro
Arylamides hybrids of two high-affinitys2 receptor ligands as tools for the development of PET radiotracers.
University of Bari Aldo Moro
Stereospecific synthesis and bio-activity of novel beta(3)-adrenoceptor agonists and inverse agonists.
University of Bari Aldo Moro
1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor.
University of Bari Aldo Moro
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.
University of Bari Aldo Moro
PB183, a sigma receptor ligand, as a potential PET probe for the imaging of prostate adenocarcinoma.
University of Bari Aldo Moro
Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
University of Bari Aldo Moro
Design and evaluation of naphthol- and carbazole-containing fluorescent sigma ligands as potential probes for receptor binding studies.
University of Bari Aldo Moro
Methyl substitution on the piperidine ring of N-[omega-(6-methoxynaphthalen-1-yl)alkyl] derivatives as a probe for selective binding and activity at the sigma(1) receptor.
University of Bari Aldo Moro
Synthesis of chiral 1-[omega-(4-chlorophenoxy)alkyl]-4-methylpiperidines and their biological evaluation at sigma1, sigma2, and sterol delta8-delta7 isomerase sites.
University of Bari Aldo Moro
Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D(3) receptor ligands.
University of Bari Aldo Moro
Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new series of high-affinity and selective ligands for the peripheral type.
University of Bari Aldo Moro
Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.
University of Bari Aldo Moro
Novel potent sigma 1 ligands: N-[omega-(tetralin-1-yl)alkyl]piperidine derivatives.
University of Bari Aldo Moro
1-aryl-4-[(1-tetralinyl)alkyl]piperazines: alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity. 3.
University of Bari Aldo Moro
New sigma and 5-HT1A receptor ligands: omega-(tetralin-1-yl)-n-alkylamine derivatives.
University of Bari Aldo Moro
Oxygen isosteric derivatives of 3-(3-hydroxyphenyl)-N-n-propylpiperidine.
University of Bari Aldo Moro
Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptorsa/¿ dual agonists.
University of Bari Aldo Moro
Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein.
University of Bari Aldo Moro
Synthesis and binding assays of novel 3,3-dimethylpiperidine derivatives with various lipophilicities ass¿? receptor ligands.
University of Bari Aldo Moro
New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function.
University of Bari Aldo Moro
Structure-based design of multitargeting ChEs-MAO B inhibitors based on phenyl ring bioisosteres: AChE/BChE selectivity switch and drug-like characterization.
University of Bari Aldo Moro
Novel 6-alkyl-bridged 4-arylalkylpiperazin-1-yl derivatives of azepino[4,3-b]indol-1(2H)-one as potent BChE-selective inhibitors showing protective effects against neurodegenerative insults.
University of Bari Aldo Moro
Development of Riluzole Analogs with Improved Use-Dependent Inhibition of Skeletal Muscle Sodium Channels.
University of Bari Aldo Moro
Development of potent isoflavone-based formyl peptide receptor 1 (FPR1) antagonists and their effects in gastric cancer cell models.
University of Bari Aldo Moro
Bioisosteric replacement based on 1,2,4-oxadiazoles in the discovery of 1H-indazole-bearing neuroprotective MAO B inhibitors.
University of Bari Aldo Moro
Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Ureidopropanamides as Formyl Peptide Receptor 2 (FPR2) Agonists to Target the Resolution of Inflammation in Central Nervous System Disorders.
University of Bari Aldo Moro
Structure-based design of novel donepezil-like hybrids for a multi-target approach to the therapy of Alzheimer's disease.
University of Bari Aldo Moro
Development of novel phenoxyalkylpiperidines as high-affinity Sigma-1 (σ
University of Bari Aldo Moro
Privileged scaffold-based design to identify a novel drug-like 5-HT
University of Bari Aldo Moro
Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor.
University of Bari Aldo Moro
Exploring Basic Tail Modifications of Coumarin-Based Dual Acetylcholinesterase-Monoamine Oxidase B Inhibitors: Identification of Water-Soluble, Brain-Permeant Neuroprotective Multitarget Agents.
University of Bari Aldo Moro
An update about the crucial role of stereochemistry on the effects of Peroxisome Proliferator-Activated Receptor ligands.
University of Bari Aldo Moro
Investigating 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole as scaffold of butyrylcholinesterase-selective inhibitors with additional neuroprotective activities for Alzheimer's disease.
University of Bari Aldo Moro
1,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1.
University of Bari Aldo Moro
Investigating alkyl nitrates as nitric oxide releasing precursors of multitarget acetylcholinesterase-monoamine oxidase B inhibitors.
University of Bari Aldo Moro
New Approaches to Cancer Therapy: Combining Fatty Acid Amide Hydrolase (FAAH) Inhibition with Peroxisome Proliferator-Activated Receptors (PPARs) Activation.
University of Bari Aldo Moro
Design, synthesis, radiolabeling and in vivo evaluation of potential positron emission tomography (PET) radioligands for brain imaging of the 5-HT₇ receptor.
University of Bari Aldo Moro
Fine molecular tuning at position 4 of 2H-chromen-2-one derivatives in the search of potent and selective monoamine oxidase B inhibitors.
University of Bari Aldo Moro
Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors.
University of Bari Aldo Moro
Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.
University of Bari Aldo Moro
Multifunctional thiosemicarbazones and deconstructed analogues as a strategy to study the involvement of metal chelation, Sigma-2 (σ
University of Bari Aldo Moro
Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation.
University of Bari Aldo Moro
Novel ureidopropanamide based N-formyl peptide receptor 2 (FPR2) agonists with potential application for central nervous system disorders characterized by neuroinflammation.
University of Bari Aldo Moro
Targets for Drug Therapy for Autism Spectrum Disorder: Challenges and Future Directions.
University of Bari Aldo Moro