A detailed structural characterization of the biologically active 1-benzylpyridinium-4-aldoxime chloride and 1-phenacylpyridinium-4-aldoxime chloride was performed using NMR and vibrational and electronic spectroscopy, as well as X-ray diffraction. The complexes of these compounds with the aquap...

Whey proteins are widely used food ingredients due to their nutritional and functional properties (gelling, emulsifying, foaming). Owning to their structure (free thiol group, lysine residues, hydrophobic pocket), they can also be used as carriers for bioactives. In this study, conjugates betwee...

Shape memory polymers play an increasingly significant role in the fields of electronics, aerospace and medical science. However, the most of shape memory polymers are derived from petroleum resource nowadays. Herein, biobased thiol-epoxy shape memory network was obtained from gallic acid-based ...

Aliphatic polyesters have been widely used in environmental and biomedical engineering, but a lack of functional groups limits their applications. Here, we reported a facile approach to synthesize vinyl functional polyester via the ring opening copolymerization of ε-caprolactone (CL) and allyl ...

Several cationic carbosilane dendrimers have been synthesized containing two different types of degradable bonds: Si–O and ester bonds. The first type of systems was prepared by reacting carbosilane dendrimers containing peripheral Si–Cl bonds with first generation dendrons presenting a –OH f...

Two directions for self-condensation of β-(isoxazol-5-yl) enamines under treatment with either acetyl chloride or acids were found leading to new 1,3-diisoxazolyl-1,3-dieneamines and 1,3,5-triisoxazolyl benzenes. The effect of solvent, acid, temperature and the reaction time on the ratio of rea...

A regioselective, solvent-free and catalyst-free synthesis of isoxazoles has been successfully developed under ball milling conditions. Milling the mixtures of N-hydroxybenzimidoyl chlorides and enamino carbonyl compounds in a ball mill at a frequency of 14.6 Hz for 20–60 min afforded isoxazole...

During the analysis of street samples for the suspected presence of controlled drugs, two samples were found to contain 4-methylamphetamine (4-MA). This is the first report of the drug in Ireland as previously only N-methylamphetamine (N-MA) had been encountered. In Ireland, little attention had...

(S)-2-(4′-[11C]methoxybiphenyl-4-sulfonylamino)-3-methylbutyric acid ([11C]MSMA) and N-hydroxy-(R)-2-[[(4′-[11C]methoxyphenyl)sulfonyl]benzylamino]-3-methylbutanamide ([11C]CGS 25966), carbon-11 labeled matrix metalloproteinase (MMP) inhibitors, have been synthesized for evaluation as new pote...

Glycidyl methacrylate (GMA), poly(GMA) and a GMA–methyl methacrylate (50–50 mol.%) random copolymer have been modified with 4-hydroxy-4’methoxy biphenyl (4H4MB) moieties through the ring opening reaction of the epoxy group with the aim of demonstrating that the occurrence of limitation of the...

Chemoenzymatic peptide synthesis is potentially the most cost-efficient technology for the synthesis of short and medium-sized peptides. However, there are still some limitations when challenging peptides, e.g. containing sterically demanding acyl donors, non-proteinogenic amino acids or proline...

The enantioselective α-amination reaction of α,α-disubstituted aldehydes can lead to a variety of enantioenriched amino aldehydes, amino alcohols, and amino acids. After screening a variety of amino acids and their derivatives, we identified a cheap, simple, commercially available aspartic ac...

N-Cbz-4,5-dehydro-l-prolineamide or N-Boc-4,5-dehydro-l-prolineamide are alternative key intermediates for the synthesis of saxagliptin, a dipeptidyl peptidase IV (DPP4) inhibitor recently approved for treatment of type 2 diabetes mellitus. An efficient biocatalytic method was developed for conv...

Application of the click reaction for coupling a 2-(2-aminoethoxy)ethoxy (AEE) function to thyminyl, cytosinyl and adeninyl peptide nucleic acid (PNA) monomer analogues bearing a N-propynyl group, in place of the original N-2-aminoethyl moiety, has been explored. The N-propynyl PNA analogues wer...

Glycine is a major inhibitory neurotransmitter and recent reports have shown that certain lipophilic derivatives of glycine demonstrate anticonvulsant activity in intact animals. In these studies, glycinamide derivatives were found to be more potent than their corresponding glycine analogues. Co...

Recent work in our laboratory has shown that the highly substituted, electronically rich 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (THIQ3CA) scaffold is a key building block for a novel class of promising anticoagulants.10 The synthesis of THIQ3CA analogs, especially containing specific, ...

γ-Glutamyl transpeptidase (GGT) catalyzing the cleavage of γ-glutamyl bond of glutathione and its S-conjugates is involved in a number of physiological and pathological processes through glutathione homeostasis. Defining its Cys-Gly binding site is extremely important not only in defining the ...

Several fully protected tri- and pentapeptides containing a central symmetrical α,α-dialkyl glycine residue, with the alkyl group varying from methyl or ethyl to benzyl, were synthesized in good yields by a strategy based on the Ugi–Passerini reaction. Each Ugi–Passerini adduct was selective...

The anticonvulsant activity of ester- and amide-type lipid conjugates of glycine and N-benzyloxycarbonylglycine (Z-glycine) was evaluated in the maximal electroshock (MES) test and the strychnine test. Regardless of the type of the conjugates the Z-glycine derivatives were always more potent tha...

A family of dipeptides consisting of proline and tert-butyl esters of amino acids, as well as simple amides of prolyl-glycine dipeptide were synthesized and tested for their organocatalytic properties on the intermolecular asymmetric aldol reaction. The peptides were tested both in organic and a...