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Concept

Combinatorial chemistry

Related publications (30)

Nickel-Catalyzed Regioselective Hydroalkylation and Hydroarylation of Alkenyl Boronic Esters

Xile Hu, Srikrishna Bera

Metal hydride catalyzed hydrocarbonation reactions of alkenes are an efficient approach to construct new carbon-carbon bonds from readily available alkenes. However, the regioselectivity of hydrocarbonation remains challenging to be controlled. In nickel h ...

Wiley-VCH Verlag GmbH2019

Manganese-mediated reductive amidation of esters with nitroarenes

Xile Hu, Peng Wang, Chi Wai Cheung, Ning Shen

Amides are ubiquitous molecules in nature and in synthetic chemistry. Here we report a convenient and efficient method to synthesize N-aryl amides via amidation of esters with nitroarenes. In the presence of manganese metal, this amidation proceeded smooth ...

ROYAL SOC CHEMISTRY2019

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK

Stewart Cole

Mycobacterium tuberculosis, the etiological agent of the infectious disease tuberculosis, kills approximately 1.5 million people annually, while the spread of multidrug-resistant strains is of great global concern. Thus, continuous efforts to identify new ...

Nature Research2018

Electrostatic spray ionization from 384-well microtiter plates for mass spectrometry analysis based enzyme assay and drug metabolism screening

Hubert Girault, Liang Qiao, Tzu-En Lin, Elena Tobolkina, Xiaoqin Zhong

We have realized the direct ionization of samples from wells of microtiter plates under atmospheric conditions for mass spectrometry analysis without any liquid delivery system or any additional interface. The microtiter plate is a commercially available 3 ...

American Chemical Society2017

Microfluidic systems for high-throughput and high-content screening using the nematode Caenorhabditis elegans

Martinus Adela Maria Gijs, Thomas Lehnert, Matteo Cornaglia

In a typical high-throughput drug screening (HTS) process, up to millions of chemical compounds are applied to cells cultured in well plates, aiming to find molecules that exhibit a robust dose-response, as evidenced for example by a fluorescence signal. I ...

Royal Soc Chemistry2017

New methods for developing (bi)cyclic peptides by phage display

Camille Villequey

Cyclic peptide ligands are a promising molecular format for the development of therapeutics. They combine some of the advantages of large protein therapeutics (high affinity and specificity) and of small molecule drugs (accessibility to chemical synthesis ...

EPFL2017

Homogeneous time-resolved G protein-coupled receptor-ligand binding assay based on fluorescence cross-correlation spectroscopy

Luc Henry

G protein-coupled receptors (GPCRs) mediate many important physiological functions and are considered as one of the most successful therapeutic target classes for a wide spectrum of diseases. Drug discovery projects generally benefit from a broad range of ...

Academic Press Inc Elsevier Science2016

Inhibiting Mycobacterium tuberculosis within and without

Stewart Cole

Tuberculosis remains a scourge of global health with shrinking treatment options due to the spread of drug-resistant strains of Mycobacterium tuberculosis. Intensive efforts have been made in the past 15 years to find leads for drug development so that bet ...

Royal Soc2016

Development of potent and selective S. aureus sortase A inhibitors Based on Peptide Macrocycles

Christian Heinis, Inmaculada Rentero Rebollo, Davide Bertoldo

Sortases are transpeptidase enzymes that anchor surface proteins, including virulence factors, to the cell wall of Gram-positive bacteria, and they are potential targets for the development of anti-infective agents. While several large compound libraries w ...

2016

Combinatorial Screening for Specific Drug Solubilizers with Switchable Release Profiles

Polymer-block-peptide conjugates are tailored to render hydrophobic small molecule drugs water soluble. The combinatorial strategy selects for bioconjugates that exhibit sequence-specific solubilization and switchable release profiles of the cargo through ...

Wiley-V C H Verlag Gmbh2015