A sulfur-containing amino acid was observed in mammalian cystine metabolism, in vitro and in vivo, which we have characterized as 2-amino, 3-(thio-thiosulfonate)propionic acid (cysteine thiosulfonate). Its biosynthetic pathway appears to initiate with the cleavage of cystine by cystathionine γ-...

The development of a new class of cysteine protease inhibitors utilising the thiosulfonate moiety as an SH specific electrophile is described. This moiety has been introduced into suitable amino acid derived building blocks, which were incorporated into peptidic sequences leading to very potent ...

Dihydro-1H-phosphole-boranes 5 and 10 were prepared from phosphine oxides 1 and 9 respectively. Reaction of borane 5 with dichlorocarbene gave dihydrophosphole-dichloromethylborane 6 and tetrahydro derivative 7a as the main products, and dichlorocyclopropane 8 as the minor component. Dichlorocar...

The 1H, 13C and 15N NMR chemical shifts of seven 2-alkylnitrosoamino-4-nitropyridines and seven 2-alkylnitrosoamino-4-nitropyridine N-oxides have been assigned. The GIAO/DFT 13C chemical shifts of energetically optimized structures have been calculated. The results were compared to the chemical ...

Nitroso-ene (NE) reactions have been adapted in the construction of nitrogen-containing motifs in many biologically interesting compounds. The transient and highly reactive “nitroso” species remains a challenge for designing stereocontrolled syntheses. Although chiral auxiliary-based method ha...

Stereochemistry of 3t,5t-Dimethyl-N-nitroso-2r,6c-bis(o-chlorophenyl) piperidin-4-one oxime (1) and 3t,5t-Dimethyl-N-nitroso-2r,6c-bis(p-chlorophenyl) piperidin-4-one oxime (2) has been studied using 1H, 13C and two-dimensional NMR spectra. Analysis of the spectral data shows that both the compo...

A number of methods are available for evaluating the potential of chemical agents to induce cancer in test animals. Recent use of SIMCA pattern recognition in structure-biological activity studies suggests that this method may be useful in making such evaluations. In this report this method is u...

The dorsal (dPAG) and ventral (vPAG) regions of the periaqueductal gray are well known to contain the neural substrates of fear and anxiety. Chemical or electrical stimulation of the dPAG induces freezing, followed by a robust behavioral reaction that has been considered an animal model of panic...

Spectroscopic and crystallographic studies show that 2-(N-(2-pyridyl)carbamoyl)pyridine (HL) in both its neutral and deprotonated forms, coordinates ruthenium(II) via the amidato- and pyridine-nitrogen atoms thereby forming five-membered rings. In neutral [Ru(HL)(PPh3)2Cl2], HL exists as a zwitt...

Correlation between Fe content and z value on the structural and magnetic properties of the Sm(CobalFexCu0.06Zr0.025)z magnets (x = 0.20, 0.25, 0.28, and z = 7, 9.5) has been investigated. It is found that the cellular phases in the magnets grow up with increasing Fe content, so the cell boundar...

α- and γ-substituted vinylthionium ions from SnCl4 ionisation of a range of substituted 1,3- and 3,3-bis (alkyl/phenylthio) propenes allylate enol allyl ethers in good yield. Levels of regioselectivity are sterically dependent and in the case of methyl as γ-substituent may be controlled by th...

A new method for the highly stereoselective synthesis of (Z) -1-phenylthio-1-trialkylsilylalkenes 3 by the elimination of methanol from 1-methoxy-1-phenylthio-1-trialkylsilylalkane 2 in organic solvents is described.

The reaction of 2-(1-alkenyl)-1,3-dithianes with the titanocene-olefin complexes, prepared by the reaction of titanocene dichloride with 2 cquiv of alkyllithiums, in the presence of triphenyl-phosphine gave 1-alkenylcyclopropanes in good yields. The similar reaction of substituted 1,3-bis(phenyl...

The novel hydrazone compound, [(E)-3-(2-nitrophenyl)-(E)-1-(2-phenylhydrazono)]-1-phenylallylidene (2), has been synthesized, characterized by FTIR, 1H NMR, 13C NMR techniques, elemental analysis, X-ray structure analysis and has been investigated gama-irradiated effect. Additionally, the molecu...

From the V2O5H2O2H2dipic–nica/pa/phen–H2O/H2OCH3CN reaction systems (H2dipic = dipicolinic acid, nica = nicotinamide, pa = picolinamide, phen = 1,10-phenanthroline), three monoperoxidovanadium(V) complexes have been synthesized and structurally characterized: (Hpa)[VO(O2)(dipic)(H2O)]⋅H2O (1),...

This study aims to develop a highly selective Lewis base adsorbent to investigate the selective sorption and recovery of Eu(III) and Sm(III) from wastewater. The oxygen and nitrogen donor atoms containing Lewis base N-methyl-N-phenyl-1,10-phenanthroline-2-carboxamide (MePhPTA) ligand was synthes...

We prepared a series of new N-[2-(4-substitutedpiperazin-1-yl)ethyl]-1-(n-butyl or phenyl)-2,5-dimethyl-3,4-pyrroledicarboximides 3 and the related products 4 and 5, nine representatives of which were evaluated as potential analgesic agents in an animal model (mice). The new pyrroledicarboximide...

An asymmetric synthesis of neurokinin substance P receptor antagonist (+)-L-733,060 starting from enantiomerically pure ethyl (R)-(+)-2,3-epoxypropanoate (ethyl glycidate) is described. The synthesis relies on a diastereoselective reductive amination, regioselective intramolecular epoxide openin...

The bioassay-guided fractionation of the aril of Myristica fragrans (mace spice) yielded five phenolic compounds, one new acyclic bis phenylpropanoid (1) and four previously known phenolic compounds: compounds (1) (S) 1-(3,4,5-trimethoxyphenyl)-2-(3-methoxy-5-(prop-1-yl) phenyl)-propan-1-ol, (2)...

Extensive ESR spin-trapping studies have shown that ethanol is oxidized to 1-hydroxyethyl radical (HER) by rat and deer mice liver microsomal systems. The ESR detection of POBN/HER nitroxide in bile, and formation of antibodies, which recognize HER adducts in alcoholics, suggest that HER is prod...