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Journal of Medicinal Chemistry

Current research reports and chronological list of recent articles..




The international scientific Journal of Medicinal Chemistry publishes studies that contribute to an understanding of the relationship between molecular structure and biological activity or mode of action.

The publisher is the American Chemical Society, ACS. The copyright and publishing rights of specialized products listed below are in this publishing house. This is also responsible for the content shown.

To search this web page for specific words type "Ctrl" + "F" on your keyboard (Command + "F" on a Mac). Then: type the word you are searching for in the window that pops up!

Additional research articles see Current Chemistry Research Articles. Magazines with similar content (medicinal chemistry):

 - Bioorganic and Medicinal Chemistry Letters,

 - European Journal of Medicinal Chemistry,

 - Journal of Enzyme Inhibition and Medicinal Chemistry,

 - Medicinal Chemistry Research.



Journal of Medicinal Chemistry - Abstracts



[ASAP] Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00180

Datum: 25.04.2018


[ASAP] Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00277

Datum: 25.04.2018


[ASAP] Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01655

Datum: 24.04.2018


[ASAP] Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00067

Datum: 24.04.2018


[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

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00210

Datum: 24.04.2018


[ASAP] Correction to Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y<sub>2</sub> Receptor Based on AR-C118925

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00606

Datum: 24.04.2018


[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)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00082

Datum: 23.04.2018


[ASAP] A Trojan-Horse Strategy Including a Bacterial Suicide Action for the Efficient Use of a Specific Gram-Positive Antibiotic on Gram-Negative Bacteria

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00522

Datum: 23.04.2018


[ASAP] Targeting Tyrosinase: Development and Structural Insights of Novel Inhibitors Bearing Arylpiperidine and Arylpiperazine Fragments

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01745

Datum: 20.04.2018


[ASAP] Combined Approach of Backbone Amide Linking and On-Resin N-Methylation for the Synthesis of Bioactive and Metabolically Stable Peptides

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01809

Datum: 20.04.2018


[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

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00041

Datum: 20.04.2018


[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

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00091

Datum: 20.04.2018


[ASAP] <sup>18</sup>F-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00240

Datum: 20.04.2018


[ASAP] Tight-Binding Inhibition of Human Monoamine Oxidase B by Chromone Analogs: A Kinetic, Crystallographic, and Biological Analysis

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00357

Datum: 20.04.2018


[ASAP] N-Substituted Prodrugs of Mebendazole Provide Improved Aqueous Solubility and Oral Bioavailability in Mice and Dogs

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01792

Datum: 19.04.2018


[ASAP] An Efficient Buchwald–Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01903

Datum: 19.04.2018


[ASAP] An <sup>18</sup>F-Labeled Poly(ADP-ribose) Polymerase Positron Emission Tomography Imaging Agent

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00138

Datum: 19.04.2018


[ASAP] Synthetic Approaches to New Drugs Approved During 2016

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00260

Datum: 19.04.2018


[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

Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00579

Datum: 19.04.2018


[ASAP] New Inhibitors of Breast Cancer Resistance Protein (ABCG2) Containing a 2,4-Disubstituted Pyridopyrimidine Scaffold

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01012

Datum: 18.04.2018


[ASAP] The Pharmacophore Network: A Computational Method for Exploring Structure–Activity Relationships from a Large Chemical Data Set

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01890

Datum: 18.04.2018


[ASAP] Hydroxamic Acids Constitute a Novel Class of Autotaxin Inhibitors that Exhibit <italic toggle="yes">in Vivo</italic> Efficacy in a Pulmonary Fibrosis Model

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00232

Datum: 18.04.2018


[ASAP] Computer-Aided Discovery and Characterization of Novel Ebola Virus Inhibitors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00035

Datum: 17.04.2018


[ASAP] Lipophilic Efficiency as an Important Metric in Drug Design

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00077

Datum: 17.04.2018


[ASAP] Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00164

Datum: 17.04.2018


[ASAP] Discovery of a Novel Small-Molecule Modulator of C–X–C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00190

Datum: 17.04.2018


[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

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00246

Datum: 17.04.2018


[ASAP] Design of Aminopeptidase N Inhibitors as Anti-cancer Agents

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b00782

Datum: 16.04.2018


[ASAP] Impact of Dynamically Exposed Polarity on Permeability and Solubility of Chameleonic Drugs Beyond the Rule of 5

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00347

Datum: 16.04.2018


[ASAP] Developing Equipotent Teixobactin Analogues against Drug-Resistant Bacteria and Discovering a Hydrophobic Interaction between Lipid II and Teixobactin

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01241

Datum: 13.04.2018


[ASAP] Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01861

Datum: 13.04.2018


[ASAP] Repurposing a Library of Human Cathepsin L Ligands: Identification of Macrocyclic Lactams as Potent Rhodesain and <italic toggle="yes">Trypanosoma brucei</italic> Inhibitors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01869

Datum: 13.04.2018


[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

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00107

Datum: 13.04.2018


[ASAP] Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT<sub>2C</sub> Receptor

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00401

Datum: 13.04.2018


[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

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00117

Datum: 12.04.2018


[ASAP] Structure–Activity Relationship Study of Cyclic Pentapeptide Ligands for Atypical Chemokine Receptor 3 (ACKR3)

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00336

Datum: 12.04.2018


[ASAP] Discovery of Novel Schizocommunin Derivatives as Telomeric G-Quadruplex Ligands That Trigger Telomere Dysfunction and the Deoxyribonucleic Acid (DNA) Damage Response

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01615

Datum: 11.04.2018


[ASAP] Organometallic Gold(III) Complexes Similar to Tetrahydroisoquinoline Induce ER-Stress-Mediated Apoptosis and Pro-Death Autophagy in A549 Cancer Cells

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01694

Datum: 11.04.2018


[ASAP] Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00170

Datum: 11.04.2018


[ASAP] Toward ß-Secretase-1 Inhibitors with Improved Isoform Selectivity

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01716

Datum: 10.04.2018


[ASAP] Synthesis and Evaluation of Hydrogen Peroxide Sensitive Prodrugs of Methotrexate and Aminopterin for the Treatment of Rheumatoid Arthritis

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01775

Datum: 10.04.2018


[ASAP] Orally Available Soluble Epoxide Hydrolase/Phosphodiesterase 4 Dual Inhibitor Treats Inflammatory Pain

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01804

Datum: 10.04.2018


[ASAP] Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01892

Datum: 10.04.2018


[ASAP] Design and Synthesis of Novel Positive Allosteric Modulators of a7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01492

Datum: 09.04.2018


[ASAP] Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01691

Datum: 09.04.2018


[ASAP] Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00116

Datum: 09.04.2018


[ASAP] Human ß-Defensin 1 and ß-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00251

Datum: 09.04.2018


[ASAP] Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01593

Datum: 06.04.2018


[ASAP] 2<italic toggle="yes">H</italic>-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.7b01870

Datum: 06.04.2018


[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 D<sub>4</sub> Receptor

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Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b00265

Datum: 06.04.2018


 


Category: Current Chemistry Research

Last update: 28.03.2018.






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