2-Hydroxyethyl methacrylate (HEMA) and N-vinylcaprolactam (NVCL) were grafted onto polypropylene films (PP) by radiation-induced grafting, using gamma-radiation (from a 60Co gamma source) with the aim of improving their surface properties and endow the films with the ability to act as drug-eluti...

Tris- 1, bis- 2, and mono- 3 (2-hydroxyethyl)amine-N-oxides isomers, their protonated forms, and H-complexes with acids have been studied in gas phase and DMSO solution by the quantum chemical calculations using DFT and MP2 methods. It is found that the proton affinity of the endo isomers 1a–3a...

Polyamide nanofiltration (NF) membranes are very sensitive to oxidant agents, and easy to be degraded by active chlorine solutions attacking. In this paper, bis-2, 6-N, N-(2-hydroxyethyl) diaminotoluene was first introduced into the preparation of polyamide NF membranes. A new type of polyamide ...

Here, the synthesis, spectral and the structural studies of 2-hydroxyethyl substituted N-heterocyclic carbene (NHC) precursors and the enzyme inhibition activities of the NHC precursors were investigated against the cytosolic carbonic anhydrase I and II isoenzymes (hCA I and hCA II), and xanthin...

1. The in vitro incubation of mussel digestive gland with 1 mM aminofluorene resulted in the formation of glucuronides that (a) became mutagenic with carp liver S9, and (b) liberated S9-dependent mutagenic aglucones after β-glucuronidase treatment.2. Natural populations of mussels from unpollut...

This work describes a method for the quantitative determination of the labile, toxic N-hydroxy metabolite of phenacetin in urine. A thin-layer chromatography step was used for the preliminary purification of extracts, and the specificity of the assay was based on the monitoring of specific metas...

The N-O-glucuronide of [14C]acetyl-N-hydroxyphenacetin is sufficiently stable to purify, but slowly breaks down in aqueous solutions to a reactive intermediate that can covalently bind to protein. When the pure compound was incubated in Tris buffer, pH 7.4, at 37°, it decomposed with a half-lif...

Inhibitors for NorA efflux pump of Staphylococcus aureus have attracted the attention of many researchers towards the discovery and development of novel efflux pump inhibitors (EPIs). In an attempt to find specific potent inhibitors of NorA efflux pump of S. aureus, a total of 15 amino acid conj...

Different strains Pseudomonas andropogonis and P. andropogonis that were previously known as “P. woodsii” and “P. stizolobii”, were grown in liquid culture and tested for the production of rhizobitoxine and hydroxythreonine. Out of 21 strains examined, 17 produced rhizobitoxine and all produ...

The synthesis of hydroxythreonine via osmylation of vinyl glycine has permitted a crystalline derivative to be prepared as well as comparison with naturally-derived material, allowing the assignment of the absolute configuration of the natural product as (2S, 3R).

Canine xenopsin and a 27 residue segment of its precursor immediately surrounding the xenopsin moiety were isolated from acidic extracts of stomach. The six C-terminal residues of canine xenopsin, H-Phe-His-Pro-Lys-Arg-Pro-Trp-Ile-Leu-OH, were identical to those in Xenopus xenopsin

The tridecapeptide neurotensin (NT) and its C-terminal homologs, including xenopsin (XP) and neuromedin N (NM-N), reduced the amplitude of spontaneous contractions in longitudinal smooth muscle strips from the porcine distal jejunum in vitro. The rank order of potency (IC50 in nM) was XP (0.1) >...

Using radioimmunoassay for detection, a mammalian counterpart to amphibian xenopsin (XP) was isolated and sequenced from pepsin-treated extracts of three different rat tissues and shown to be H-Phe-His-Pro-Lys-Arg-Pro-Trp-Ile-Leu-OH. This peptide, which shares six of the eight residues in XP, ex...

Two avian counterparts to amphibian xenopsin have been identified as H-Phe-His-Pro-Lys-Arg-Pro-Trp-Ile-Leu-OH (XP-2) and its partial sequence H-His-Pro-Lys-Arg-Pro-Trp-Ile-Leu-OH (XP-1) isolated from extracts of turkey proventriculus and skin. Both peptides were shown to be present within these ...

Lysates of isolated rat polymorphonuclear leukocytes and macrophages were found to generate xenopsin-related peptides when incubated with a liver extract used as a source of precursor. The lysosomal enzyme, cathepsin D, was also shown to display this property and to share with the lysate a simil...

5-(Phenylthiophene)-3-carboxylic acid (2a), a metabolite of esonarimod (1), which was developed as a new antirheumatic drug, was considered as a lead compound for new antirheumatic drugs. A new series of 2a derivatives were synthesized and their characteristic pharmacological effects, that is th...

The reaction of 1-bromo-2-(1-isothiocyanatoalkyl)benzenes, which are easily derived from 2-bromophenyl ketones or (2-bromophenyl)methanamine, with butyllithium generates 1-(1-isothiocyanatoalkyl)-2-lithiobenzenes, which immediately underwent intramolecular cyclization to give rise to the corresp...

A series of (±)-trans-dihydronarciclasine and (±)-trans-dihydrolycoricidine derivatives with variously substituted ring A was synthesised and evaluated for their antiproliferative activity against 60 human tumour cell lines (NCI60), representing leukemia, melanoma, and cancers of the lung, col...

During our search for topically-active Caspase-1 inhibitors, we identified a novel class of potent inhibitors based on a 1,3,5-trisubstituted uracil motif equipped with an l-aspartate semi-aldehyde derived warhead. In the literature, the majority of Caspase-1 inhibitors possessing the same warhe...

The infrared spectra (3200–50 cm−1) of gaseous and solid and Raman spectra (3200–10 cm−1) of the liquid with qualitative depolarization ratios and solid 3-bromo-3,3-difluoropropene CH2CHCBrF2 have been recorded. Both the gauche and cis conformers have been identified in the fluid phase, but th...