Journal of Medicinal Chemistry

[ASAP] Insights into the Mechanism of Antimicrobial Activity of Seven-Residue Peptides (Fri, 17 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00353
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[ASAP] 2-Phenylquinoline <italic toggle="yes">S. aureus</italic> NorA Efflux Pump Inhibitors: Evaluation of the Importance of Methoxy Group Introduction (Fri, 17 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00791
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[ASAP] Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity (Fri, 17 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01013
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[ASAP] Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer (Thu, 16 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00224
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[ASAP] Synergistic Multiresidue Substitutions of a Macrocyclic c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-<sc>d</sc>Pro] Agouti-Related Protein (AGRP) Scaffold Yield Potent and >600-Fold MC4R versus MC3R Selective Melanocortin Receptor Antagonists (Thu, 16 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00684
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[ASAP] Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((<italic toggle="yes">S</italic>)-2,2-Difluorocyclopropyl)((1<italic toggle="yes">R</italic>,5<italic toggle="yes">S</italic>)-3-(2-((1-methyl-1<italic toggle="yes">H</italic>-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841) (Thu, 16 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00917
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[ASAP] Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties (Wed, 15 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00450
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[ASAP] Chemoenzymatic Synthesis and Pharmacological Characterization of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid Transporter Inhibitors (Wed, 15 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00700
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[ASAP] Synthesis and Activity of a Novel Autotaxin Inhibitor–Icodextrin Conjugate (Wed, 15 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00935
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[ASAP] Resurrection Biology: Aged Acetylcholinesterase Brought Back to Life (Wed, 15 Aug 2018)
Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01122
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[ASAP] Thermodynamics of DNA Minor Groove Binders<subtitle>Perspective</subtitle> (Tue, 14 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00233
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[ASAP] Sulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant <italic toggle="yes">Staphylococcus aureus</italic> (MRSA) (Tue, 14 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00989
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[ASAP] Conformational Propensity and Biological Studies of Proline Mutated LR Peptides Inhibiting Human Thymidylate Synthase and Ovarian Cancer Cell Growth (Mon, 13 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01699
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[ASAP] Structural Optimization and Characterization of Potent Analgesic Macrocyclic Analogues of Neurotensin (8–13) (Mon, 13 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00175
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[ASAP] Molecular Imaging of Sirtuin1 Expression–Activity in Rat Brain Using Positron-Emission Tomography–Magnetic-Resonance Imaging with [<sup>18</sup>F]-2-Fluorobenzoylaminohexanoicanilide (Mon, 13 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00253
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[ASAP] Synthesis, Characterization, and Biological Evaluation of a Porphyrin-Based Photosensitizer and Its Isomer for Effective Photodynamic Therapy against Breast Cancer (Fri, 10 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00547
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[ASAP] Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1) (Fri, 10 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b01007
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[ASAP] 5-Aroylindoles Act as Selective Histone Deacetylase 6 Inhibitors Ameliorating Alzheimer’s Disease Phenotypes (Thu, 09 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00151
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[ASAP] Discovery of Novel 1,3,8-Triazaspiro[4.5]decane Derivatives That Target the c Subunit of F<sub>1</sub>/F<sub>O</sub>-Adenosine Triphosphate (ATP) Synthase for the Treatment of Reperfusion Damage in Myocardial Infarction (Thu, 09 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00278
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[ASAP] Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents (Thu, 09 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00664
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[ASAP] Allosteric Modulators of HSP90 and HSP70: Dynamics Meets Function through Structure-Based Drug Design (Thu, 09 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00825
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[ASAP] A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1<italic toggle="yes">H</italic>,2<italic toggle="yes">H</italic>,3<italic toggle="yes">H</italic>-pyrrolo[3,2-<italic toggle="yes">b</italic>]pyridin-1-yl)-2-[(2<italic toggle="yes">R</italic>,5<italic toggle="yes">R</italic>)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660) (Thu, 09 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00900
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[ASAP] Design, Synthesis, and Biological Evaluation of Novel 7-[(3<italic toggle="yes">aS</italic>,7<italic toggle="yes">aS</italic>)-3<italic toggle="yes">a</italic>-Aminohexahydropyrano[3,4-<italic toggle="yes">c</italic>]pyrrol-2(3<italic toggle="yes">H</italic>)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens (Wed, 08 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00644
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[ASAP] Surface Probing by Fragment-Based Screening and Computational Methods Identifies Ligandable Pockets on the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase (Wed, 08 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00842
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[ASAP] Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure–Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept (Tue, 07 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00782
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[ASAP] Salicylic Acid Derivatives Inhibit Oxalate Production in Mouse Hepatocytes with Primary Hyperoxaluria Type 1 (Mon, 06 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00399
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[ASAP] Yeast Chemogenomic Profiling Reveals Iron Chelation To Be the Principle Cell Inhibitory Mode of Action of Gossypol (Mon, 06 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00692
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[ASAP] From Naproxen Repurposing to Naproxen Analogues and Their Antiviral Activity against Influenza A Virus (Fri, 03 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00557
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[ASAP] Polypharmacology by Design: A Medicinal Chemist’s Perspective on Multitargeting Compounds (Fri, 03 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00760
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[ASAP] Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1<italic toggle="yes">H</italic>-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK) (Thu, 02 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00807
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[ASAP] Biguanide Iridium(III) Complexes with Potent Antimicrobial Activity (Thu, 02 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00906
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[ASAP] Development of Novel Monoamine Oxidase-B (MAO-B) Inhibitors with Reduced Blood–Brain Barrier Permeability for the Potential Management of Noncentral Nervous System (CNS) Diseases (Wed, 01 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01588
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[ASAP] Identification of the 4-Position of 3-Alkynyl and 3-Heteroaromatic Substituted Pyridine Methanamines as a Key Modification Site Eliciting Increased Potency and Enhanced Selectivity for Cytochrome P-450 2A6 Inhibition (Wed, 01 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00084
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[ASAP] Discovery of ß-Arrestin Biased Ligands of 5-HT<sub>7</sub>R (Wed, 01 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00642
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[ASAP] Design, Synthesis, and SAR of C-3 Benzoic Acid, C-17 Triterpenoid Derivatives. Identification of the HIV-1 Maturation Inhibitor 4-((1<italic toggle="yes">R</italic>,3a<italic toggle="yes">S</italic>,5a<italic toggle="yes">R</italic>,5b<italic toggle="yes">R</italic>,7a<italic toggle="yes">R</italic>,11a<italic toggle="yes">S</italic>,11b<italic toggle="yes">R</italic>,13a<italic toggle="yes">R</italic>,13b<italic toggle="yes">R</italic>)-3a-((2-(1,1-Dioxidothiomorpholino)ethyl)amino)-5a,5b,8,8,11a-pentamethyl-1-(prop-1-en-2-yl)-2,3,3a,4,5,5a,5b,6,7,7a,8,11,11a,11b,12,13,13a,13b-octadecahydro-1<italic toggle="yes">H</italic>-cyclopenta[<italic toggle="yes">a</italic>]chrysen-9-yl)benzoic Acid (GSK3532795, BMS-955176) (Wed, 01 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00854
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[ASAP] From Oxiranes to Oligomers: Architectures of U.S. FDA Approved Pharmaceuticals Containing Oxygen Heterocycles (Wed, 01 Aug 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00876
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[ASAP] Recent Advances in the Medicinal Chemistry of Liver X Receptors<subtitle>Miniperspective</subtitle> (Mon, 30 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00045
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[ASAP] Structure–Function Analysis of Immune Checkpoint Receptors to Guide Emerging Anticancer Immunotherapy (Mon, 30 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00541
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[ASAP] Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-? (ROR? or RORc) Inhibitors: Hits and Misses (Mon, 30 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00588
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[ASAP] Lead-like Drugs: A Perspective<subtitle>Miniperspective</subtitle> (Fri, 27 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00407
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[ASAP] <italic toggle="yes">Pseudomonas aeruginosa</italic> Quorum Sensing Systems as Drug Discovery Targets: Current Position and Future Perspectives (Fri, 27 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00540
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[ASAP] Identification of the First Synthetic Allosteric Modulator of the CB<sub>2</sub> Receptors and Evidence of Its Efficacy for Neuropathic Pain Relief (Mon, 23 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00368
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[ASAP] Collagen Prolyl 4-Hydroxylase as a Therapeutic Target<subtitle>Miniperspective</subtitle> (Mon, 23 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00822
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[ASAP] Why Are the Majority of Active Compounds in the CNS Domain Natural Products? A Critical Analysis (Fri, 20 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.7b01922
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[ASAP] Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics (Fri, 20 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00185
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[ASAP] Identification of Thiourea-Based Inhibitors of the B-Cell Lymphoma 6 BTB Domain via NMR-Based Fragment Screening and Computer-Aided Drug Design (Tue, 17 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00040
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[ASAP] Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction (Tue, 17 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00294
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[ASAP] De Novo Design, Synthesis, and Biological Evaluation of 3,4-Disubstituted Pyrrolidine Sulfonamides as Potent and Selective Glycine Transporter 1 Competitive Inhibitors (Tue, 17 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00295
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[ASAP] Monoacylglycerol Acyltransferase 2 (MGAT2) Inhibitors for the Treatment of Metabolic Diseases and Nonalcoholic Steatohepatitis (NASH)<subtitle>Miniperspective</subtitle> (Tue, 17 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00864
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[ASAP] Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure–Functional Selectivity Relationships (SFSRs) and Therapeutic Potential (Tue, 10 Jul 2018)
TOC Graphic Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.8b00435
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