Journal of Medicinal Chemistry

Bacterial Iron Uptake Pathways: Gates for the Import of Bactericide Compounds (Fri, 28 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00554
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Design, Synthesis, and Evaluation of Novel 2,6-Disubstituted Phenol Derivatives as General Anesthetics (Fri, 28 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00254
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Design, Synthesis, and Evaluation of a Series of Novel Benzocyclobutene Derivatives as General Anesthetics (Fri, 28 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00253
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Selective IKur Inhibitors for the Potential Treatment of Atrial Fibrillation: Optimization of the Phenyl Quinazoline Series Leading to Clinical Candidate 5-[5-Phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl]pyridine-3-sulfonamide (Fri, 28 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01889
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Pyrazolopyrimidines as Potent Stimulators for Transient Receptor Potential Canonical 3/6/7 Channels (Fri, 28 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00304
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Correction to Design of Potent and Druglike Nonphenolic Inhibitors for Catechol O-Methyltransferase Derived from a Fragment Screening Approach Targeting the S-Adenosyl-l-methionine Pocket (Thu, 27 Apr 2017)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00613
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Prediction of Antibiotic Interactions Using Descriptors Derived from Molecular Structure (Thu, 27 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00204
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Determination of in Vitro and in Silico Indexes for the Modeling of Blood–Brain Barrier Partitioning of Drugs via Micellar and Immobilized Artificial Membrane Liquid Chromatography (Thu, 27 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01811
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First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases (Thu, 27 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00062
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Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis (Wed, 26 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01703
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Transforming Sphingosine Kinase 1 Inhibitors into Dual and Sphingosine Kinase 2 Selective Inhibitors: Design, Synthesis, and in Vivo Activity (Tue, 25 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00233
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Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair (Tue, 25 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00271
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Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis (Tue, 25 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01718
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How Frequently Are Pan-Assay Interference Compounds Active? Large-Scale Analysis of Screening Data Reveals Diverse Activity Profiles, Low Global Hit Frequency, and Many Consistently Inactive Compounds (Tue, 25 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00154
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A Tobramycin Vector Enhances Synergy and Efficacy of Efflux Pump Inhibitors against Multidrug-Resistant Gram-Negative Bacteria (Mon, 24 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00156
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Development of an Acrylate Derivative Targeting the NLRP3 Inflammasome for the Treatment of Inflammatory Bowel Disease (Mon, 24 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01624
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Amphiphilic Tobramycin–Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline (Mon, 24 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01742
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Synthesis and Characterization of Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Antibacterial Activity against Gram-Negative Bacteria (Mon, 24 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01831
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Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors (Mon, 24 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00357
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Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents (Mon, 24 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01834
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Slow but Steady Wins the Race: Dissimilarities among New Dual Inhibitors of the Wild-Type and the V27A Mutant M2 Channels of Influenza A Virus (Mon, 24 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01758
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Past, Current, and Future Developments of Therapeutic Agents for Treatment of Chronic Hepatitis B Virus Infection (Fri, 21 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01442
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Predicting “Hot” and “Warm” Spots for Fragment Binding (Fri, 21 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00366
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Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors (Fri, 21 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00017
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A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos (Thu, 20 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01921
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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities (Thu, 20 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01851
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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity (Thu, 20 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01850
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Nitrile in the Hole: Discovery of a Small Auxiliary Pocket in Neuronal Nitric Oxide Synthase Leading to the Development of Potent and Selective 2-Aminoquinoline Inhibitors (Wed, 19 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00259
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Second Generation Triple-Helical Peptide Inhibitors of Matrix Metalloproteinases (Wed, 19 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00018
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Addressing Structural Flexibility at the A-Ring on Salvinorin A: Discovery of a Potent Kappa-Opioid Agonist with Enhanced Metabolic Stability (Wed, 19 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00148
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Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants (Tue, 18 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00172
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Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals) (Mon, 17 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01872
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A “Click Chemistry Platform” for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation (Mon, 17 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01781
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Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure–Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1 (Thu, 13 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01911
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Sustainable Practices in Medicinal Chemistry Part 2: Green by Design (Wed, 12 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01837
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CNS Physicochemical Property Space Shaped by a Diverse Set of Molecules with Experimentally Determined Exposure in the Mouse Brain (Fri, 07 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01469
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Targeted Antibiotic Delivery: Selective Siderophore Conjugation with Daptomycin Confers Potent Activity against Multidrug Resistant Acinetobacter baumannii Both in Vitro and in Vivo (Sat, 01 Apr 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00102
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Modulators of Sphingosine-1-phosphate Pathway Biology: Recent Advances of Sphingosine-1-phosphate Receptor 1 (S1P1) Agonists and Future Perspectives (Thu, 30 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01575
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Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor (Wed, 29 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00113
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Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery (Mon, 27 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01287
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Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression (Fri, 24 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01816
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Embarking on a Chemical Space Odyssey (Fri, 24 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b00423
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Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives (Wed, 15 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01595
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Structural Analysis of Chemokine Receptor–Ligand Interactions (Fri, 10 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01309
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Drug Discovery Targeting Bromodomain-Containing Protein 4 (Thu, 02 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01761
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Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors (Thu, 02 Mar 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01543
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Regulating the Master Regulator: Controlling Ubiquitination by Thinking Outside the Active Site (Tue, 28 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01346
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A Drug of Such Damned Nature.1 Challenges and Opportunities in Translational Platinum Drug Research (Tue, 28 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01351
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Bitopic Ligands and Metastable Binding Sites: Opportunities for G Protein-Coupled Receptor (GPCR) Medicinal Chemistry (Wed, 15 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01601
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4-Hydroxyphenylpyruvate Dioxygenase and Its Inhibition in Plants and Animals: Small Molecules as Herbicides and Agents for the Treatment of Human Inherited Diseases (Tue, 14 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01395
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The Necessary Nitrogen Atom: A Versatile High-Impact Design Element for Multiparameter Optimization (Wed, 08 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01807
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Inhibitors of Influenza Virus Polymerase Acidic (PA) Endonuclease: Contemporary Developments and Perspectives (Tue, 07 Feb 2017)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01227
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