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12 09 2019
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Microwave-assisted diastereoselective two-step three-component synthesis for rapid access to drug-like libraries of substituted 3-amino-b-lactams

Large, diverse compound libraries are an essential requisite in target-based drug development. In...

12 09 2019
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Synthesis by Click Reactions and Antiplasmodial Activity of Lupeol 1,2,3-Triazole Derivatives

Lupeol, a triterpene frequently found in Asteraceae plant species, showed moderate to low activity...

12 09 2019
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Highly Potent, Stable, and Selective Dimeric Hetarylpropylguanidine-Type Histamine H2 Receptor Agonists

On the basis of the long-known prototypic pharmacophore 3-(1H-imidazol-4-yl)propylguanidine (SK&F...

12 09 2019
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The flexible cytoplasmic loop 3 contributes to the substrate affinity of human monocarboxylate transporters

Human monocarboxylate transporters (hMCTs/SLC16As) mediate the transport of small molecular weight...

12 09 2019
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2‐Phenylquinoline S. aureus NorA Efflux Pump Inhibitors: Evaluation of the Importance of Methoxy Group Introduction

Antimicrobial resistance (AMR) represents a hot topic in drug discovery. Besides the identification...

12 09 2019
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Organoarsenicals in poultry litter: Detection, fate, and toxicity

Arsenic contamination in groundwater has endangered the health and safety of millions of people...

12 09 2019
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Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors

A series of 31 N,N-disubstituted 2-amino-5-halomethyl-2-thiazolines was designed, synthesized, and...

12 09 2019
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Far-Red and Near-Infrared Seminaphthofluorophores for Targeted Pancreatic Cancer Imaging

Molecular probes that selectively highlight pancreatic cancer (PC) tissue have the potential to...

12 09 2019
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Temperature-Dependent Estimation of Gibbs Energies Using an Updated Group-Contribution Method

Reaction-equilibrium constants determine the metabolite concentrations necessary to drive flux...

12 09 2019
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A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation

Ethionamide (ETH) is one of the most widely used second-line chemotherapeutic drugs for the...

12 09 2019
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Novel medium-throughput technique for investigating drug-cyclodextrin complexation by pH-metric titration using the partition coefficient method

The present study was aimed to develop a medium-throughput screening technique for investigation of...

12 09 2019
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Characterization of the Penetration of the Blood–Brain Barrier by High-Performance Liquid Chromatography (HPLC) Using a Stationary Phase with an Immobilized Artificial Membrane

The biological activity of drugs on organisms is associated with the pharmacokinetic properties,...