Acetyl CoA:arylamine N-acetyltransferase (NAT) enzymes catalyze the N-acetylation of aromatic amines and the O-acetylation of aryl hydroxylamines, reactions that govern the disposition and toxicity of many drugs and carcinogens. The human NAT genes and enzymes NAT1 and NAT2 are highly polymorphic and constitute one of the best studied examples of the genetic control of drug metabolism. Naturall...

calix(6)arene hydroxamic acids (iii) are synthesised for the first time by reactingcalix(6)arene acid chloride(ii) with substituted hydroxylamines at low temperature in the presence ofsodium bicarbonate. the p-carboxycalix(6)arene(i) is obtained by an acid catalysed condensationreaction of p-hydroxybenzoic acid and formaldehyde. these calixarenes are characterised by meltingpoint, uv, ir, 1h nm...

(1)H NMR of two H(2)@C(60) nitroxide derivatives has been characterized indirectly by reducing to their corresponding hydroxylamines. Nuclear spin relaxation of the endohedral H(2) and external protons of the H(2)@C(60) nitroxide and its corresponding hydroxylamine were measured and analyzed. The observed spectra are consistent with negligible scalar coupling between the unpaired electron and t...

A copper-catalyzed regioselective and stereospecific aminoboration of vinylsilanes with bis(pinacolato)diboron (pinB-Bpin) and hydroxylamines has been developed. In the presence of a CuCl/MeO-dppbz catalyst, the boryl group and amino group are incorporated at the β position and α position, respectively, and the corresponding β-boryl-α-aminosilanes are obtained with good diastereoselectivity. Th...

Due to its inherent reactivity, nitroxyl (HNO), must be generated in situ through the use of donor compounds, but very few physiologically useful HNO donors exist. Novel N-substituted hydroxylamines with carbon-based leaving groups have been synthesized, and their structures confirmed by X-ray crystallography. These compounds generate HNO under nonenzymatic, physiological conditions, with the r...

A novel NIS-mediated oxidative cyclization of N-(2-trifluoromethyl-3-alkynyl)hydroxylamines is developed, which provides a facile access to 4-trifluoromethyl-5-acylisoxazoles in 33-91% yields. Various types of commonly used electrophilic halogen source such as ICl, I2, NIS, NBS and NCS at different temperatures in various solvents were investigated. It was found that the NIS acts as both an oxi...

Monoprotonated aliphatic hydroxylamines, acetone oxime, and dimethyl sulfoxide as their fluoroantimonate salts (prepared from the corresponding hydrochloric acid salts) in SbF5-SOzClF (or SOz) solution were studied to determine the site of protonation. Subsequently, diprotonation was also investigated in HSOsF-SbFs (magic acid) solution. From the 'H and 13C NMR data of the static and exchanging...

H(2)O@C(60) derivatives covalently linked to a nitroxide radical were synthesized. The (1)H NMR of the guest H(2)O revealed the formation of many isomers with broad signals. Reduction to the diamagnetic hydroxylamines sharpened the (1)H NMR signals considerably and allowed for an "isomer count" based on the number of observed distinct signals. For H(2)O@K-8, 17 positional isomeric nitroxides ar...