We investigated insecticidal effects of iminoctadine liquid formulation, a fungicide containing iminoctadine triacetate, on the silkworm Bombyx mori that is an important domesticated insect. Iminoctadine liquid formulation was incorporated in an artificial diet and fed to silkworms for 24 h on t...

Iminoctadine tris (albesilate) is a bis-guazatine fungicide, and its specific modes of action and efficacy against C. cassiicola are not yet clear. In this study, baseline sensitivity data for mycelial growth showed that the frequency distribution curve of iminoctadine tris (albesilate) EC50 val...

There is a body of evidence implying the involvement of the central glutamatergic system in morphine dependence. In this study, we examined the effect of intracerebroventricular (i.c.v.) administration of a potent glutamate transporter inhibitor, dl-threo-β-benzyloxyaspartate (dl-TBOA), on acut...

Selected 3JHH coupling constants and theoretical calculations were used to explain the conformational equilibrium of L-tryptophan methyl ester (Trp-OMe) in several solvents. The obtained 3JHαHβ values did not exhibit any significant variability and thus indicate that there are no conformationa...

A series of N-{para-(ferrocenyl) ethynyl benzoyl} amino acid and dipeptide methyl and ethyl esters 4–18 were prepared by coupling para-(ferrocenyl) ethynyl benzoic acid 3 to the amino acids GABA(OMe), GABA(OEt) and the dipeptide esters GlyGly(OMe), GlyGly(OEt), Gly-L-Ala(OMe), Gly-L-Ala(OEt), G...

A straightforward synthesis of a series of new catalysts derived from N-triphenylmethyl-aziridine-2-carbohydrazides is described. The new compounds have been tested for the enantioselective addition of diethyl- and phenylethynylzinc to aryl and alkyl aldehydes, which afforded the corresponding c...

The roots of four species of Zanthoxylum were examined for the presence of zanthoxylol (2-dimethylallyl-4-(3-hydroxy-propyl)phenol) but only Z. zanthoxyloides was found to contain this substance. Purification was effected using Sephadex ionexchange resins; isolation and quantification were perfo...

The endonuclease III from Escherichia coli is a repair enzyme which exhibits both a glycosylase and an endonuclease functions. The activity of the enzyme can be assayed by measuring the released targeted bases in solution from a sample of modified DNA. In the present study, gas chromatography–m...

When two solutions of cis-6-hydroperoxy-5-hydroxy-5,6-dihydrothymine and ascorbic acid in deuterium oxide were mixed, chemically induced dynamic nuclear polarization was observed. The reaction gave N-formyl-N′-pyruvylurea.

The structure of cis-5-hydroperoxy-6-hydroxy-5,6-dihydrothymine was obtained using X-ray crystallography [space group P21n (Z = 4) with a = 11.428(2) Å, b = 6.284(1) Å, c = 11.882(2) Å and β = 110.56(3) °]. Electronic properties of the thymine hydroxyhydroperoxide were determined, both in t...

The development of a new FRET OFF → ON system to the colorimetric and ratiometric sensing of azide ions is described. The sensor is based on an oxazolone-pyrimidinone dyad, containing both oxazolone and pyrimidinone linked through a conjugated triazole spacer prepared by Copper (I) catalyzed [3...

A new, simple thermally efficient and solvent-free condensation of 2-amino-3-cyano-6-methyl-4-phenyl-4H-pyran-5-ethylcarboxylate derivatives with coumarin-3-carboxylic acid employing pentafluorophenylammonium triflate (PFPAT) as an inexpensive organocatalyst for the synthesis of a series of ethy...

A method for the construction of fluorinated pyrimidinones based on the reaction of cyanodifluoromethyl-substituted amines with isocyanates is described. The use of ortho-iodophenylisocyanate in this reaction followed by copper catalyzed intramolecular amination affords fluorinated fused heteroc...

A direct regioselective Csp2–H trifluoromethylation of pyrimidinones and pyridinones using CF3SO2Na/Mn(OAc)3 to afford 5-trifluoromethyl pyrimidinones and 3-trifluoromethyl pyridinones in moderate to good yields was described. The reaction showed that the steric hindrance due to bulky groups ad...

In this study, the synthesis of some new 5-acetyl-3,4-dihydro-6-methyl-4-(substituted phenyl)-2(1H)-pyrimidinones has been reported. The compounds were prepared by the Biginelli reaction of acetylacetone with aromatic aldehydes and urea. The structures of the compounds were characterized by UV, ...

A new class of 2(1H)-pyrimidinone derivatives was identified as potential EGFR T790M inhibitors against TKI-resistant NSCLC. These novel compounds inhibited the EGFR T790M kinase activity at concentrations in the range of 85.3 to 519.9 nM. In particular, compound 7e exhibited the strongest activ...

The molecular complex between 1-(2-methoxyphenyl)-1H-imidazole-2(3H)-thione (HmimOMe) and iodine (I2) was investigated. Single crystal of [(HmimOMe)I2] adduct was grown by slow evaporation technique from chloroform at room temperature. Spectroscopic techniques such as FT-IR and Raman techniques,...

Rat alpha-fetoprotein (AFP) contains a site that both binds the protease substrate tryptophan methyl ester (TrpOMe) and influences estrogen binding. We have studied the effect of changing the amino acid and ester portions of this compound on its binding to AFP, as measured by the ability of the ...

A base labile urethane (Bnpeoc) group derived from 2,2-bis(4′-nitrophenyl)ethan-1-ol has been developed as an amine protecting group. This protecting group may be cleaved using the reagents DBN, DBU, DBU/HOAc and piperidine. The preparations of Nα-Bnpeoc amino acids and applications to peptide...

A simple, RRLC–ESI-MS/MS method was developed for the simultaneous determination of five oleanane pulchinenosides (B3, BD, B7, B10, and B11), in rat plasma following solid-phase extraction (SPE). Detection and quantitation were performed by MS/MS using electrospray ionization (ESI) and multiple...