Synthetic human pancreastatin (1–52) and its C-terminal fragment (24–52) were first evaluated with respect to the biological activity on the insulin secretion in the isolated rat islets. Both these pancreastatins inhibited glucose-stimulated insulin secretion at a concentration of 100 nM. The ...

Circulating molecular forms with pancreastatin (PST)-like immunoreactivity in plasma from normal subjects were examined. An immunoreactive form corresponding to a human PST-like sequence [human chromogranin-A-(250–301)] (hPST-52) and a larger form (mol wt 15–21 kDa) were detected by gel filtra...

We examined the in vitro degradation of human pancreastatin-52 (hPST-52) and a larger molecular form (approximate 15 kDa) of human PST by an enzyme extract from human kidney. The PST-degrading activity was determined from the amount of immunoreactive PST remaining after incubation of hPST-52 or ...

In this study, a series of novel thiazolidin-4-ones (5a–g) and azetidin-2-ones (6a–g) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl)hydrazine carboxamide derivatives of the benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gra...

The synthesis of a series of 3-(p-substituted phenylazo)-6-pyridone dyes, which are suitable for the dyeing of polyester fabrics, is described. Characterisation of the dyes was carried out by spectral and elemental analysis. The colour parameters of the dyed fabrics were measured. The assessment...

The state of the tautomeric equilibria of eleven arylazo pyridone dyes was evaluated from UV–Vis absorption spectra with the aid of the quantum mechanical modeling. NMR analysis and theoretical calculations, by using PCM/ωB97X-D/6-311G(d,p) method, confirmed that prepared compounds exist mainl...

Thermal degradation properties of 5-(4-substitutedphenylazo)-3-amido-6-hydroxy-4-methyl-2-pyridones and 5-(4-substitutedphenylazo)-3-cyano-6-hydroxy-4-methyl-2-pyridones dyes, differing in electron withdrawing and electron donating substituents in para-position of diazo components were examined....

The electrochemical behavior of six arylazo pyridone dyes classified to the substituents present at the phenylazo and 2-pyridone moiety and their 1:1 inclusion complexes with (2-hydroxypropyl)-β-cyclodextrin was studied using cyclic and square wave voltammetry in 0.1 M NaOH on a gold electrode....

A series of novel 5-(4-substituted phenylazo)-1-carboxymethyl-3-cyano-6-hydroxy-4-methyl-2-pyridones had been synthesized and characterized. The study includes spectral determination of the possible tautomeric forms and the intramolecular hydrogen bonding pattern. The influence of the bifurcated...

Twelve different derivatives of substituted-{5-[2-(1,2,3,4-tetrahydrocarbazol-9-yl)ethyl]tetrazol-1-yl}alkanones (3–14) were synthesized by reacting 9-[2-(1H-tetrazol-5-yl)-ethyl]-2,3,4,9-tetrahydro-1H-carbazole (2) and the appropriate acid chlorides. 9-[2-(1H-tetrazol-5-yl) ethyl]-2,3,4,9-tetr...

1-(5-Chloroindol-3-yl)-3-hydroxy-3-(2H-tetrazol-5-yl)-propenone (5CITEP) is an inhibitor of the HIV-1 integrase (IN). Theoretical studies were performed on the interaction of this inhibitor with surrounding amino acids. Density functional theory (DFT) calculations were conducted to identify the ...

The present study describes the discovery and characterization of a series of 5-aryl-2H-tetrazol-3-ylacetamides as G protein-gated inwardly-rectifying potassium (GIRK) channels activators. Working from an initial hit discovered during a high-throughput screening campaign, we identified a tetrazo...

N-Acetonylation of 5(3)-(1H-tetrazol-1-yl)-3(5)-nitro-1H-pyrazole with bromoacetone in the presence of NaHCO3 at 60 °C gave, along with expected isomeric N-acetonyl derivatives, a tricyclic product of the intramolecular electrophilic attack at the carbon atom of the tetrazole cycle.

The stability and the stereoselectivity of newly prepared n-pentyl 1-methyl-1H-tetrazol-5-yl (MT) sulfone 1a in the Julia-Kocienski reactions were compared with those of the PT sulfone 1b and the TBT sulfone 1c. The improved stability of the anion derived from the n-pentyl MT sulfone 1a enhanced...

Optically active α-(tetrazol-1-yl)-substituted carboxylic acid OBO-esters were synthesized from the corresponding a-isocyano OBO-esters and trimethylsilyl azide in up to 92% yield. Subsequent acidic hydrolysis proceeds without epimerization and makes it possible to prepare enantiomerically pure...

2-(1H-Tetrazol-1-yl)thiazole (tth), prepared by heterocyclization of 2-aminothiazole with triethyl orthoformate and sodium azide, was found to react with copper(II) chloride in ethanol giving a mixture of [Cu(tth)2Cl2]n (1) and [Cu2(ethc)2Cl4]·2H2O (2), where ethc is ethyl thiazol-2-ylcarbamimi...

A series of novel 5-methoxy-2,3-naphthalimide derivatives were designed, synthesized and evaluated for their biological activities. In particular, the ability of the compounds to synergize with antimicrobials, to inhibit Nile Red efflux, and to target AcrB was assayed. The results showed that th...

Reactions of 2-R-3-nitro-2H-chromenes (R=CF3, CCl3, Ph) with aminoenones derived from acetylacetone and cyclic amines (morpholine, piperidine) proceed diastereoselectively to give mainly cis–trans-2,3,4-trisubstituted chromanes as a result of nucleophilic addition of the vinylogous β-methyl gr...

A new regioselective method for the synthesis of 2-aryl-5-benzoylpyridine derivatives has been developed. The reaction proceeds via ring opening and closing cascade mechanism (ROCC) of isoxazole to synthesize various functionalized pyridine derivatives. This is the first report for the preparati...

The Suzuki cross-coupling between 2-(4-bromophenyl)-5-chloropyrazine and a range of aryl boronic acids has been investigated. The regioselectivity of the reaction can be switched between the aryl bromide and pyrazinyl chloride positions by changing the ligand associated with the palladium cataly...