64 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Improved Potency of Indole-Based NorA Efflux Pump Inhibitors: From Serendipity toward Rational Design and Development.
University of Perugia
Metabolism study and biological evaluation of bosentan derivatives.
University of Perugia
Polymerase Acidic Protein-Basic Protein 1 (PA-PB1) Protein-Protein Interaction as a Target for Next-Generation Anti-influenza Therapeutics.
University of Perugia
Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.
University of Perugia
Indole Based Weapons to Fight Antibiotic Resistance: A Structure-Activity Relationship Study.
University of Perugia
Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.
University of Perugia
One-pot heterogeneous synthesis of¿(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors.
University of Perugia
Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors.
University of Perugia
Design, synthesis, crystallographic studies, and preliminary biological appraisal of new substituted triazolo[4,3-b]pyridazin-8-amine derivatives as tankyrase inhibitors.
University of Perugia
Asymmetric synthesis of the four diastereoisomers of a novel non-steroidal farnesoid X receptor (FXR) agonist: role of the chirality on the biological activity.
University of Perugia
Re-evolution of the 2-phenylquinolines: ligand-based design, synthesis, and biological evaluation of a potent new class of Staphylococcus aureus NorA efflux pump inhibitors to combat antimicrobial resistance.
University of Perugia
Comparison of ligand-based and structure-based 3D-QSAR approaches: a case study on (aryl-)bridged 2-aminobenzonitriles inhibiting HIV-1 reverse transcriptase.
University of Perugia
Inhibitor of ovarian cancer cells growth by virtual screening: a new thiazole derivative targeting human thymidylate synthase.
University of Perugia
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
University of Perugia
Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists.
University of Perugia
Synthesis and biological affinity of new imidazo- and indol-arylpiperazine derivatives: further validation of a pharmacophore model for alpha(1)-adrenoceptor antagonists.
University of Perugia
Synthesis, molecular modeling studies, and preliminary pharmacological characterization of all possible 2-(2'-sulfonocyclopropyl)glycine stereoisomers as conformationally constrained L-homocysteic acid analogs.
University of Perugia
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.
University of Perugia
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.
University of Perugia
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.
University of Perugia
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.
University of Perugia
Farnesoid X receptor: from structure to potential clinical applications.
University of Perugia
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid.
University of Perugia
Smart region definition: a new way to improve the predictive ability and interpretability of three-dimensional quantitative structure-activity relationships.
University of Perugia
Modulation of the kynurenine pathway in search for new neuroprotective agents. Synthesis and preliminary evaluation of (m-nitrobenzoyl)alanine, a potent inhibitor of kynurenine-3-hydroxylase.
University of Perugia
Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR).
University of Perugia
Design, synthesis and preliminary evaluation of novel 3'-substituted carboxycyclopropylglycines as antagonists at group 2 metabotropic glutamate receptors.
University of Perugia
A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.
University of Perugia
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3a,7a-dihydroxy-6a-ethyl-24-nor-5β-cholan-23-amine.
University of Perugia
Inhibitors of ABCG2-mediated multidrug resistance: Lead generation through computer-aided drug design.
University of Perugia
Virtual screening for novel openers of pancreatic K(ATP) channels.
University of Perugia
Small Molecules Targeting DNA Polymerase Theta (POLθ) as Promising Synthetic Lethal Agents for Precision Cancer Therapy.
University of Perugia
Development of 3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-sulfate sodium salt (INT-767): Process optimization, synthesis and characterization of metabolites.
University of Perugia
Identification of Human Alanine-Glyoxylate Aminotransferase Ligands as Pharmacological Chaperones for Variants Associated with Primary Hyperoxaluria Type 1.
University of Perugia
Discovery of 2-Phenylquinolines with Broad-Spectrum Anti-coronavirus Activity.
University of Perugia
Medicinal Chemistry Perspective on Targeting Mono-ADP-Ribosylating PARPs with Small Molecules.
University of Perugia
Potent 2,3-dihydrophthalazine-1,4-dione derivatives as dual inhibitors for mono-ADP-ribosyltransferases PARP10 and PARP15.
University of Perugia
1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors.
University of Perugia
Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
University of Perugia
Synthesis and characterization of 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide-based compounds targeting the PA-PB1 interface of influenza A virus polymerase.
University of Perugia
Modulating microRNA Processing: Enoxacin, the Progenitor of a New Class of Drugs.
University of Perugia
The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology.
University of Perugia
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
University of Perugia
Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists.
University of Perugia
Discovery of potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation.
University of Perugia
Targeting Aryl hydrocarbon receptor for next-generation immunotherapies: Selective modulators (SAhRMs) versus rapidly metabolized ligands (RMAhRLs).
University of Perugia
Scaffold hopping approach on the route to selective tankyrase inhibitors.
University of Perugia
New pyrazolobenzothiazine derivatives as hepatitis C virus NS5B polymerase palm site I inhibitors.
University of Perugia
Discovery of novel and cardioselective diltiazem-like calcium channel blockers via virtual screening.
University of Perugia
Calcium channel antagonists discovered by a multidisciplinary approach.
University of Perugia
GBR compounds and mepyramines as cocaine abuse therapeutics: chemometric studies on selectivity using grid independent descriptors (GRIND).
University of Perugia
Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.
University of Perugia
GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors.
University of Perugia
Potent 6-desfluoro-8-methylquinolones as new lead compounds in antibacterial chemotherapy.
University of Perugia
Pharmacophore-Based Repositioning of Approved Drugs as Novel Staphylococcus aureus NorA Efflux Pump Inhibitors.
University of Perugia
Targeting Wnt-driven cancers: Discovery of novel tankyrase inhibitors.
University of Perugia
Functionalized 2,1-benzothiazine 2,2-dioxides as new inhibitors of Dengue NS5 RNA-dependent RNA polymerase.
University of Perugia
Studies on 2-phenylquinoline Staphylococcus aureus NorA efflux pump inhibitors: New insights on the C-6 position.
University of Perugia
2-Phenylquinoline S. aureus NorA Efflux Pump Inhibitors: Evaluation of the Importance of Methoxy Group Introduction.
University of Perugia
Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.
University of Perugia
Fragment-based approach to identify IDO1 inhibitor building blocks.
University of Perugia