Herein, we are reporting a rapid one-pot synthesis of MoS2-decorated laser-induced graphene (MoS2-LIG) by direct writing polyimide foils. By covering the polymer surface with layer MoS2 dispersion before processing, it is possible to obtain an in situ decoration porous network during laser writing. The resulting material three-dimensional arrangement agglomerated and wrinkled flakes decorated nanosheets good electrical properties high area, suitable be employed as electrodes for...

Stretchable electrochemical supercapacitor exploiting laser-induced graphene (LIG) transfer onto elastomeric substrates is reported. Elastomeric energy-storage devices are fabricated using polymeric electrolyte and all-PDMS (all-polydimethylsiloxane) architecture. The symmetric LIG/PDMS can sustain repeated charge–discharge cycles without suffering significant deterioration of specific capacitance even under stretching bending conditions. As a service to our authors readers, this journal...

Recently a series of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives bearing different substituents were synthesized and screened pharmacologically in order to evaluate their central nervous system activity. The purpose this study was the effects title compounds on CNS activity by varying thiadiazole moiety. It found that some these possess marked antidepressant anxiolytic properties comparable efficiency reference drugs Imipramine Diazepam. most potent compound 3k further investigated...

Rac1 protein is implicated in several events of atherosclerotic plaque development and represents a new potential pharmacological target for cardiovascular diseases. In this paper we describe pharmacophore virtual screening followed by molecular docking calculations leading to the identification five inhibitors. These compounds were shown be more effective than reference compound NSC23766 reducing intracellular levels Rac1-GTP, thus supporting approach

Allenamides of α-amino acids were converted into enantiopure 2-vinylimidazolidin-4-ones by a carbopalladation/exo-cyclization process. The products obtained in 2.5:1−5.5:1 dr, with 94−99% ee. palladium-catalyzed carbonylative cyclization the same substrates afforded enone structures. Starting from properly substituted allenamides, an intramolecular carbopalladation followed amination gave rise to tricyclic fused-ring imidazolidinones.

The purpose of this work is to set up a general protocol for the production antimicrobial materials based on cellulose and peptides. We exploited chemical ligation reaction achieve conjugation peptides cellulose; aim, we produced thioester cysteine-modified cellulose. As handle can be inserted at any position peptide, peptide immobilized onto through its N- or C-terminal end other within sequence. Our experiments performed Escherichia coli cultures show that conjugated lasioglossin-III...

The use of the 2-amino-3-(phenylsulfanyl)norbornane-2-carboxylate scaffold has been exploited for de novo design potent Rac1 inhibitors acting as modulators protein–protein interaction between and Tiam1. A series compounds differing in regio- stereochemistry prepared by way a multistep synthesis based on cycloaddition reactions Pd chemistry. Pharmacological analyses showed that all were active selective Rac1, most effective compound 13 was capable inhibiting smooth muscle cell migration....

A very efficient synthesis of orthogonally protected 1H-azepine-4-amino-4-carboxylic acid, abbreviated as Azn, a conformationally restricted analogue ornithine, was realized. It obtained on gram scale in good overall yield five steps, three which did not require isolation the intermediates, starting from readily available 1-amino-4-oxo-cyclohexane-4-carboxylic acid. Both enantiomers were used for preparation pentapeptide models containing Ala, Aib, and Azn. Conformational studies using both...

“Environmentally sustainable” synthesis of a new enantiopure morpholino β-amino acid from glucose: tool for exotic peptide architectures.

Through a computational approach, five new compounds with potent and selective Rac inhibitory activity were identified. In particular, compound 4 was shown to selectively inhibit in concentration-dependent manner by affecting the GEF-dependent GDP–GTP exchange. This more than original inhibitors previously

A new α,α-disubstituted constrained glutamine analogue has been designed to decorate gold nanoparticles and induce a 310-helix when inserted in peptides. Using an efficient "one-pot" asymmetric Schmidt reaction between 4-disubstituted-cyclohexanone hydroxyalkylazides, 1H-azepine-2-oxo-5-amino-5-carboxylic acid was prepared. The main (R) isomer at the N-terminus very short peptide sequence (i.e., PhCO-(R)-Oxo-Azn-l-Ala-Aib-l-AlaNHMe) stable conformation obtained, as verified by both NMR...

A small library of six polarity-sensitive fluorescent dyes, nicknamed MediaChrom, was prepared. This class dyes is characterized by a pyrimidoindolone core fitted out with conjugated push-pull system and carboxy linker for conceivable coupling biomolecules. The optimized eight-step synthetic strategy involves highly chemo- regioselective gold-catalyzed cycloisomerization reaction. photophysical properties MediaChrom have been evaluated in-depth. In particular, the bearing diethylamino as an...

Two model peptides containing the 3-benzylsulfanylnorbornene amino acid (NRB) was prepared. Theoretical calculations, spectroscopic and X-ray analyses confirmed that both NRB enantiomers possess a strong right-handed helicogenic effect.

We investigate the electrospinning of small molecules, specifically designed peptide derivatives pyrazole-isothiazole scaffold. Such non-natural peptides enhance spectrum fundamental materials used for electrospinning. Unlike standard electrospun materials, our are not polymeric, but able to aggregate in solution and especially during processing. They contain donor/acceptor groups that can form hydrogen bonds, generate π-stacking interactions, which known as important requirements assembly...

The exploitation of self-assembled systems to improve the solubility drugs is getting more and attention. Among different types biomaterials, peptides in particular containing non-coded amino acids (NCAPs) are promising because their use opens door stable materials inducing increased stability proteolysis. New classes NCAP, Ac-Ala-X-Ala-Aib-AlaCONH2 (X = alpha-aminoisobutyric acid (Aib) or X cyclopentane (Ac5c)) have been prepared correlation between secondary peptide structure solvent (i.e....

Poor colloidal stability of gold nanoparticles (AuNPs) in physiological environments remains one the major limitations that contribute to their difficult translation from bench clinic. For this reason, an active research field is development molecules able hamper AuNPs aggregation tendency environments. In context, synthetic peptides are gaining increased interest as alternative use biomacromolecules and polymers, due easiness synthesis profitable pharmacokinetic profile. work, we reported...

A tetrahydro-4H-(pyrrolo[3,4-d]isoxazol-3-yl)methanamine scaffold was designed as a diamino derivative to stabilize parallel turn conformations. Its synthesis took advantage of [1,3]-dipolar cycloaddition reaction between the nitrile oxide derived from inexpensive enantiopure l-phenylalanine and N-benzyl-3-pyrroline. Two diastereoisomers were formed, whose distribution depends on selected base. 3aR,6aS-Isomer is favored in organic bases, which formation driven by π-interactions. However,...