Anilines 1a-h on reaction with potassium thiocyanate and bromine in acetic acid yielded substituted 2-amino[2,1-b][1,3]benzothiazoles 3a-h. The compounds 3a-h on reaction with ethyl acetoacetate and pheylidine acetoacetate, yielded, 2-methyl-4-H-pyrimido[2,1b][1,3]benzothiazole-4-ones 4a-h and ethyl 4-phenyl-2-methyl-4H–pyrimido[2,1b][1,3]benzothiazole-3-carboxylates 5a-h respectively. Pheylidi...

Contrary to the limited effects of alkyl amides and their corresponding N-derivatives, alkyl amines affected both gram-positive and gram-negative organisms. As with other alkyl derivatives the most sensitive gram-negative bacteria were usually more resistant than the most resistant gram-positive bacteria. Compounds with a chain-length of 11 to 15 are most active. Although some of the general pr...

Cantharidin is a natural compound of novel structure with ideal insecticidal activity. However, the relationship of structure to insecticidal activity of cantharidin and its derivatives has not been ever clarified. To explore what determines the insecticidal activity structurally of cantharidin-related compounds, two series target compounds 6 and 7 were synthesized by replacing the anhydride ri...

While N-heterocyclic carbenes (NHC) are ubiquitous ligands in catalysts for organic or industrial synthesis, their potential to form transition metal complexes for medicinal applications has still to be exploited. Within this frame, new Au(I)-NHC compounds have been synthesized and structurally characterized via different methods. The solid state structure of one of these compounds was also est...

Transition metal-catalyzed asymmetric hydrogenation of heteroaromatic compounds is undoubtedly a straightforward and environmentally friendly method for the synthesis of a wide range of optically active heterocyclic compounds, which are widespread and ubiquitous in naturally occurring and artificial bioactive molecules. Over the past decade, a number of transition metal (Ir, Rh, Ru, and Pd) cat...

Abstract Here, we present a thorough structural study of small, easily accessible amino−organolithium compounds with bridging phenyl and naphthyl moieties. Their crystal structures most likely represent their aggregation as tetramers dimers in both hydrocarbon ethereal solvents. These were further used to generate corresponding aluminium model system. are reported too. All discussed focus on th...

Among the multiple factors that induce Alzheimer's disease, aggregation of the amyloid β peptide (Aβ) is considered the most important due to the ability of the 42-amino acid Aβ peptides (Aβ1-42) to form oligomers and fibrils, which constitute Aβ pathological aggregates. For this reason, the development of inhibitors of Aβ1-42 pathological aggregation represents a field of research interest. Se...

High nitrate and amine-rich food intake may result in an increased risk of endogenous formation of carcinogenic N-nitroso compounds (NOCs). We studied the eVects of whole strawberries, garlic and kale on the formation of N-nitrosodimethylamine (NDMA) in a traditional Korean diet (amine and nitrate-rich) in simulated saliva and gastric conditions. The addition of whole strawberries, kale and gar...

RATIONALE An isotopic labeling strategy based on derivatizing amine-containing metabolites has been developed using light ((12) C6 ) and heavy ((13) C6 ) N-benzoyloxysuccinimide reagents for semi-targeted metabolomic applications. METHODS Differentially labeled samples were combined and analyzed simultaneously by liquid chromatography/high-resolution tandem mass spectrometry (LC/HR-MS/MS) to ...

Thirty-two psychotropic substances were listed as designated substances (Shitei-Yakubutsu, 31 compounds and 1 plant) in Japan by the Pharmaceutical Affairs Law in April 2007 for preventing the abuse of these substances. Subsequently, other psychoactive compounds were also added to this category, 40 substances (classified as 12 tryptamines, 17 phenethylamines, 3 piperazines, 6 alkyl nitrites, 1 ...