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Themed collection Editors' Collection: Fluorine chemistry in medicinal chemistry and chemical biology

18 items
Open Access Review Article

Recent advances in direct trifluoromethylation of olefinic C–H bonds

The aim of this review is to provide a comprehensive overview of the direct trifluoromethylation of olefinic C–H bonds with special attention on the mechanistic aspects of the reactions.

Graphical abstract: Recent advances in direct trifluoromethylation of olefinic C–H bonds
Open Access Review Article

Recent advances in the synthesis of fluorinated hydrazones

Fluorinated compounds are widely used in pharmaceuticals, agrochemicals, and materials.

Graphical abstract: Recent advances in the synthesis of fluorinated hydrazones
Open Access Paper

Translational incorporation of modified phenylalanines and tyrosines during cell-free protein synthesis

E. coli wild-type translational machinery utilizes a range of nonproteinogenic amino acids for protein synthesis with incorporation levels greater than 95%.

Graphical abstract: Translational incorporation of modified phenylalanines and tyrosines during cell-free protein synthesis
Open Access Paper

Rhenium(I) complexation–dissociation strategy for synthesising fluorine-18 labelled pyridine bidentate radiotracers

A novel fluorine-18 radiolabelling method employing rhenium(I) mediation is described herein. In less than 1 minute, fluorine-18 labelled complexes and ligands were synthesised in greater than 80% and 60% radiochemical yields (RCY), respectively.

Graphical abstract: Rhenium(i) complexation–dissociation strategy for synthesising fluorine-18 labelled pyridine bidentate radiotracers
Open Access Paper

2′-Fluoro-c-di-GMP as an oral vaccine adjuvant

2′-F-c-di-GMP was synthesized through the modified H-phosphonate chemistry. 2′-F-c-di-GMP was found to be an effective mucosal vaccine adjuvant, both intranasally and orally.

Graphical abstract: 2′-Fluoro-c-di-GMP as an oral vaccine adjuvant
Open Access Paper

3(2H)-pyridazinone derivatives: a new scaffold for novel plant activators

Due to the emergence of drug resistance, pesticide residue and environmental contamination, it is important to develop novel eco-friendly strategies to protect plants.

Graphical abstract: 3(2H)-pyridazinone derivatives: a new scaffold for novel plant activators
Open Access Paper

Combinatorial synthesis and biological evaluations of (E)-β-trifluoromethyl vinylsulfones as antitumor agents

(E)-β-Trifluoromethyl vinylsulfones is accomplished through a reaction of alkynes, Togni reagent, and sodium benzenesulfinates under metal-free conditions. p-Acetylphenyl in R1 has the best activities against several tumor cells.

Graphical abstract: Combinatorial synthesis and biological evaluations of (E)-β-trifluoromethyl vinylsulfones as antitumor agents
Open Access Paper

Synthesis, structural studies and biological properties of some phosphono-perfluorophenylalanine derivatives formed by SNAr reactions

Several novel phosphono-perfluorophenylalanine derivatives, as mimetics of phenylalanine, were synthesized by subjecting diethyl (2-(perfluorophenyl)-1-(phenylamino)ethyl)-phosphonate to SNAr reactions with thiols, amines and phenols.

Graphical abstract: Synthesis, structural studies and biological properties of some phosphono-perfluorophenylalanine derivatives formed by SNAr reactions
Open Access Paper

Fluorination and chlorination effects on quinoxalineimides as an electron-deficient building block for n-channel organic semiconductors

Three fluorinated or chlorinated quinoxalineimide units (QI-1F, QI-2F, and QI-2Cl) have been designed and developed.

Graphical abstract: Fluorination and chlorination effects on quinoxalineimides as an electron-deficient building block for n-channel organic semiconductors
Open Access Paper

Fully automated peptide radiolabeling from [18F]fluoride

A fully automated approach for peptide radiolabeling from [18F]fluoride, provides an efficient process that is amenable to GMP production of [18F]F-peptide radiotracers.

Graphical abstract: Fully automated peptide radiolabeling from [18F]fluoride
Open Access Paper

19 F multiple-quantum coherence NMR spectroscopy for probing protein–ligand interactions

An NMR experiment is presented that allows identification of weak binders typically found in early stages of drug discovery programs.

Graphical abstract: 19F multiple-quantum coherence NMR spectroscopy for probing protein–ligand interactions
Open Access Paper

N α -arylsulfonyl histamines as selective β-glucosidase inhibitors

A selective β-glucosidase inhibitor was discovered using the chemically engineered extracts approach.

Graphical abstract: Nα-arylsulfonyl histamines as selective β-glucosidase inhibitors
Open Access Paper

Chemoenzymatic synthesis of polypeptides in neat 1,1,1,2-tetrafluoroethane solvent

Chemoenzymatic polypeptide synthesis offers several advantages over chemical or other biological routes, however, the use of aqueous-based media suffers from reverse hydrolysis reactions that challenge peptide chain propagation.

Graphical abstract: Chemoenzymatic synthesis of polypeptides in neat 1,1,1,2-tetrafluoroethane solvent
Open Access Paper

Sulfur(VI) fluoride exchange as a key reaction for synthesizing biaryl sulfate core derivatives as potent hepatitis C virus NS5A inhibitors and their structure–activity relationship studies

SuFEx chemistry was utilized for the design and synthesis of potent HCV NS5A inhibitors featuring a biaryl sulfate core.

Graphical abstract: Sulfur(vi) fluoride exchange as a key reaction for synthesizing biaryl sulfate core derivatives as potent hepatitis C virus NS5A inhibitors and their structure–activity relationship studies
Open Access Paper

Design and virtual screening of novel fluoroquinolone analogs as effective mutant DNA GyrA inhibitors against urinary tract infection-causing fluoroquinolone resistant Escherichia coli

Design and development of novel fluoroquinolones analogs using target (mutant DNA GyrA), ligand-based SAR and virtual screening techniques.

Graphical abstract: Design and virtual screening of novel fluoroquinolone analogs as effective mutant DNA GyrA inhibitors against urinary tract infection-causing fluoroquinolone resistant Escherichia coli
Open Access Paper

Trifluoromethylated proline analogues as efficient tools to enhance the hydrophobicity and to promote passive diffusion transport of the L-prolyl-L-leucyl glycinamide (PLG) tripeptide

The incorporation of trifluoromethylated proline analogues in the tripeptide PLG enhances its hydrophobicity and promotes passive diffusion transport.

Graphical abstract: Trifluoromethylated proline analogues as efficient tools to enhance the hydrophobicity and to promote passive diffusion transport of the l-prolyl-l-leucyl glycinamide (PLG) tripeptide
Open Access Paper

Click chemistry approaches to expand the repertoire of PEG-based fluorinated surfactants for droplet microfluidics

Click-synthesis of fluorinated surfactants for droplet microfluidics.

Graphical abstract: Click chemistry approaches to expand the repertoire of PEG-based fluorinated surfactants for droplet microfluidics
Open Access Paper

Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety

Novel trifluoromethyl pyridine derivatives bearing 1,3,4-oxadiazole whereas synthesized, their which showed good insecticidal activity; a 3D-QSAR model with good predictability was is proposed.

Graphical abstract: Design, synthesis, insecticidal activity and 3D-QSR study for novel trifluoromethyl pyridine derivatives containing an 1,3,4-oxadiazole moiety
18 items

About this collection

This collection, guest-edited by Professor Norio Shibata (Nagoya Institute of Technology), features articles published in the journal on fluorine chemistry related to medicinal chemistry and chemical biology.

Organofluorine compounds are revealed in the extensive use of key materials in diverse industrial areas of pharmaceuticals, agrochemicals, specialty materials, and polymers. In particular, the high demand for organofluorine compounds on the drug market has been evidenced by the sharp increase in the number of fluoro-pharmaceuticals approved each year. Fluorine-related papers published in the journal span over various research fields, including synthetic methodology, medicinal chemistry, chemical biology, and materials science.

We hope you will enjoy one of the states of the art of fluorine chemistry by this collection.

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