A series of 3-chloroquinoxaline-2-carboxamides were designed and prepared by the condensation of 3-chloro-2-quinoxaloylchloride with appropriate Mannich bases of the p-aminophenol in the microwave environment. The synthesized compounds were evaluated for serotonin(3) (5-HT(3)) receptor antagonistic activities in longitudinal muscle-myenteric plexus (LMMP) preparation from guinea pig ileum again...

Two new phenylpropanoid glycosides named cuneataside E (1) and cuneataside F (2), were isolated from the aerial parts of Lespedeza cuneata (Dum. Cours.) G. Don, whose structures were E and Z isomer, respectively. Their structures were elucidated on the basis of comprehensive spectroscopic analysis (UV, IR, HR-ESI-MS, 1D and 2D NMR). In in vitro bioassays at 10 μmol/L, compound 1 showed moderate...

Indandione 1 was brominated to yield 2-bromoIndandione 2 which on further reacted with substituted thiocarbamides, carbamides, 2-aminothiophenols, 2-aminophenol and triazoles to furnished 3-substituted aniline-2-thia-4-aza-6,7-benzo-8-oxo-bicyclo [3.3.0]-1(5),3-octadiene 3, 3-substituted aniline-2-oxa-4-aza-6,7-benzo-8-oxo-bicyclo [3.3.0]-1(5),3-octadiene 4, 2-Thia-5-aza-9-oxo-3,4-(3’-substitut...

The combinatorial synthesis of 2-aminophenoxazin-3-one (APO) in a microfluidic device is reported. Individual microfluidic chips containing metallic zinc, silica-immobilized hydroxylaminobenzene mutase and silica-immobilized soybean peroxidase are connected in series to create a chemo-enzymatic system for synthesis. Zinc catalyzes the initial reduction of nitrobenzene to hydroxylaminobenzene wh...

The mechanism of reduction of p-nitrosophenol (pNSP) catalyzed by horse liver alcohol dehydrogenase (HADH) and human a-alcohol dehydrogenase (a-ADH) has been compared in transient and steady-state experiments. Our results indicate that pNSP reduction catalyzed by these two ADH proceeds by different mechanisms. In one mechanism, shown by Equation 1, pNSP is reduced to p-aminophenol (PAP) via tw...

The oxidative ring cleavage of aromatic substrates by nonheme Fe dioxygenases is thought to involve formation of a ferrous-(substrate radical) intermediate. Here we describe the synthesis of the trigonal-bipyramdial complex Fe((Ph2)Tp)(ISQ(tBu)) (2), the first synthetic example of an iron(II) center bound to an iminobenzosemiquinonate (ISQ) radical. The unique electronic structure of this S = 3...

BACKGROUND Hair dye products constitute an important source of allergen exposure, and contribute importantly to allergic contact dermatitis in consumers and hairdressers. OBJECTIVES To evaluate the presence of potent contact sensitizers in oxidative hair dye products intended for home use on the US market. METHODS Ingredient labels of 107 hair dyes from 10 major brands were examined and use...

The ability of the liver to form glucuronides was measured in 10 patients with infectious hepatitis. One test was done at the onset and another about four weeks later after the clinical symptoms had disappeared. N-acetyl-p-aminophenol (N.A.P.A.) or acetanilide was administered in doses ranging from 10 to 20 mg. per kg. body weight, either orally or by intravenous injection. N.A.P.A. is conjugat...

We developed an automated colorimetric method for the quantitative determination of p-aminophenol with a Cobas Mira analyzer. The procedure can be used for the biological monitoring of human exposure to aniline. An absorbed aniline dose is extensively oxidized to p-aminophenol, which is excreted in urine mainly as glucurono- and sulfo- conjugates. After enzymatic hydrolysis, we reacted the free...