Journal of Medicinal Chemistry

[ASAP] Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne (Tue, 24 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00067
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[ASAP] Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFß) Production in Regulatory T-Cells (Tue, 24 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00210
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[ASAP] Highlights of the Structure–Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530) (Mon, 23 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00082
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[ASAP] A Trojan-Horse Strategy Including a Bacterial Suicide Action for the Efficient Use of a Specific Gram-Positive Antibiotic on Gram-Negative Bacteria (Mon, 23 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00522
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[ASAP] Targeting Tyrosinase: Development and Structural Insights of Novel Inhibitors Bearing Arylpiperidine and Arylpiperazine Fragments (Fri, 20 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01745
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[ASAP] Combined Approach of Backbone Amide Linking and On-Resin N-Methylation for the Synthesis of Bioactive and Metabolically Stable Peptides (Fri, 20 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01809
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[ASAP] Ligand–Phospholipid Conjugation: A Versatile Strategy for Developing Long-Acting Ligands That Bind to Membrane Proteins by Restricting the Subcellular Localization of the Ligand (Fri, 20 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00041
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[ASAP] Strategic Approaches to Overcome Resistance against Gram-Negative Pathogens Using ß-Lactamase Inhibitors and ß-Lactam Enhancers: Activity of Three Novel Diazabicyclooctanes WCK 5153, Zidebactam (WCK 5107), and WCK 4234 (Fri, 20 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00091
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[ASAP] ¹⁸F-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management (Fri, 20 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00240
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[ASAP] Tight-Binding Inhibition of Human Monoamine Oxidase B by Chromone Analogs: A Kinetic, Crystallographic, and Biological Analysis (Fri, 20 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00357
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[ASAP] N-Substituted Prodrugs of Mebendazole Provide Improved Aqueous Solubility and Oral Bioavailability in Mice and Dogs (Thu, 19 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01792
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[ASAP] An Efficient Buchwald–Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration (Thu, 19 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01903
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[ASAP] An ¹⁸F-Labeled Poly(ADP-ribose) Polymerase Positron Emission Tomography Imaging Agent (Thu, 19 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00138
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[ASAP] Synthetic Approaches to New Drugs Approved During 2016 (Thu, 19 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00260
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[ASAP] Correction to Discovery, Structure–Activity Relationship, and Binding Mode of an Imidazo[1,2-<italic toggle="yes">a</italic>]pyridine Series of Autotaxin Inhibitors (Thu, 19 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00579
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[ASAP] New Inhibitors of Breast Cancer Resistance Protein (ABCG2) Containing a 2,4-Disubstituted Pyridopyrimidine Scaffold (Wed, 18 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01012
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[ASAP] The Pharmacophore Network: A Computational Method for Exploring Structure–Activity Relationships from a Large Chemical Data Set (Wed, 18 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01890
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[ASAP] Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit <italic toggle="yes">in Vivo</italic> Efficacy in a Pulmonary Fibrosis Model (Wed, 18 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00232
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[ASAP] Computer-Aided Discovery and Characterization of Novel Ebola Virus Inhibitors (Tue, 17 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00035
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[ASAP] Lipophilic Efficiency as an Important Metric in Drug Design (Tue, 17 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00077
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[ASAP] Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361) (Tue, 17 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00164
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[ASAP] Discovery of a Novel Small-Molecule Modulator of C–X–C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis (Tue, 17 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00190
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[ASAP] Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, ß-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation (Tue, 17 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00246
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[ASAP] Design of Aminopeptidase N Inhibitors as Anti-cancer Agents (Mon, 16 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00782
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[ASAP] Impact of Dynamically Exposed Polarity on Permeability and Solubility of Chameleonic Drugs Beyond the Rule of 5 (Mon, 16 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00347
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[ASAP] Developing Equipotent Teixobactin Analogues against Drug-Resistant Bacteria and Discovering a Hydrophobic Interaction between Lipid II and Teixobactin (Fri, 13 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01241
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[ASAP] Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity (Fri, 13 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01861
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[ASAP] Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and <italic toggle="yes">Trypanosoma brucei</italic> Inhibitors (Fri, 13 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01869
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[ASAP] Structural Modification of Natural Product Ganomycin I Leading to Discovery of a a-Glucosidase and HMG-CoA Reductase Dual Inhibitor Improving Obesity and Metabolic Dysfunction in Vivo (Fri, 13 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00107
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[ASAP] Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT_2C Receptor (Fri, 13 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00401
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[ASAP] Discovery of a Potent (4<italic toggle="yes">R</italic>,5<italic toggle="yes">S</italic>)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling (Thu, 12 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00117
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[ASAP] Structure–Activity Relationship Study of Cyclic Pentapeptide Ligands for Atypical Chemokine Receptor 3 (ACKR3) (Thu, 12 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00336
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[ASAP] Discovery of Novel Schizocommunin Derivatives as Telomeric G-Quadruplex Ligands That Trigger Telomere Dysfunction and the Deoxyribonucleic Acid (DNA) Damage Response (Wed, 11 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01615
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[ASAP] Organometallic Gold(III) Complexes Similar to Tetrahydroisoquinoline Induce ER-Stress-Mediated Apoptosis and Pro-Death Autophagy in A549 Cancer Cells (Wed, 11 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01694
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[ASAP] Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1 (Wed, 11 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00170
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[ASAP] Toward ß-Secretase-1 Inhibitors with Improved Isoform Selectivity (Tue, 10 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01716
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[ASAP] Synthesis and Evaluation of Hydrogen Peroxide Sensitive Prodrugs of Methotrexate and Aminopterin for the Treatment of Rheumatoid Arthritis (Tue, 10 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01775
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[ASAP] Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain (Tue, 10 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01804
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[ASAP] Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones (Tue, 10 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01892
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[ASAP] Design and Synthesis of Novel Positive Allosteric Modulators of a7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice (Mon, 09 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01492
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[ASAP] Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria (Mon, 09 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01691
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[ASAP] Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors (Mon, 09 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00116
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[ASAP] Human ß-Defensin 1 and ß-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors (Mon, 09 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00251
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[ASAP] Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors (Fri, 06 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01593
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[ASAP] 2<italic toggle="yes">H</italic>-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design (Fri, 06 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01870
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[ASAP] 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D₄ Receptor (Fri, 06 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00265
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[ASAP] Correction to Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor (Fri, 06 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00475
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[ASAP] Synthesis and Structure–Activity Relationships of the Novel Antimalarials 5-Pyridinyl-4(1<italic toggle="yes">H</italic>)-Pyridones (Thu, 05 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01256
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[ASAP] Antitubercular Bis-Substituted Cyclam Derivatives: Structure–Activity Relationships and in Vivo Studies (Thu, 05 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01569
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[ASAP] Chemogenomic Profiling of Human and Microbial FK506-Binding Proteins (Thu, 05 Apr 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00137
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