ATP-sensitive potassium (KATP) channel openers have a relaxation effect due to the lower cellular membrane potential and inhibit calcium influx. There has been considerable interest in exploring KATP channel openers in the treatment of various diseases such as cardiovascular, cerebrovascular, and urinary system disease and premature labor. The purpose of this study was to synthesize 3,3,6,6-tet...

The aryl hydrocarbon receptor (AhR) is a ligand-activated basic-helix-loop-helix transcription factor that binds polyaromatic hydrocarbons (PAH), such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), and mediates their toxicity. Binding of PAH to AhR in the cytoplasm triggers a poorly defined transformation step of the receptor into a nuclear transcription factor. In this study, we show that the ...

Abstract We report the synthesis of 4‐aryl‐2‐piperidone, 4‐arylpiperidine motifs, antituberculosis molecule Q203 (Telacebec) and its analogues. Direct lactamization β ‐C−H arylated N ‐phthaloyl δ ‐aminopentanoic acid carboxamides yielded 4‐aryl‐2‐piperidone (4‐aryl‐ ‐valerolactam) scaffolds. The required were assembled via Pd(II)‐catalyzed, 8‐aminoquinoline‐aided, sp 3 activation arylation meth...

synthesis of 4-(n,n- dimethylamino)-3-aryl-3-butene-2-one, ethyl-5-aryl-4-oxo-4h-pyran-2-carboxylate, ethyl-5-aryl-4-pyridones-2-carboxylate and 5-aryl-3-cyano-5-methyl-2-pyridones (aryl=3-thienyl, 2-furyl) are described.

Reactions of the aryl complexes Rh(aryl){? 3 -P,O,P-[xant(P i Pr 2 ) ]} (1; = 3,5-Me C 6 H (a), 5 (b), 3,5-Cl (c), 3-FC 4 (d); xant(P 9,9-dimethyl-4,5-bis-(diisopropylphosphino)xanthene) with O , CO, and MeO CC?CCO Me have been performed. Under 1 atm pentane solutions afford dinuclear peroxide derivatives [Rh(aryl){? -P,P-xant(P }] (?-O (2a–2d) as yellow solids. In solution, these species are u...

BACKGROUND/AIMS Homovanillamine is a biogenic amine that it is catalyzed to homovanillyl aldehyde by monoamine oxidase A and B, but the oxidation of its aldehyde to the acid derivative is usually ascribed to aldehyde dehydrogenase and a potential contribution of aldehyde oxidase and xanthine oxidase is usually ignored. METHODS The present investigation examines the metabolism of homovanillami...

BACKGROUND/AIMS The oxidation of xenobiotic-derived aromatic aldehydes with freshly prepared liver slices has not been previously reported. The present investigation compares the relative contribution of aldehyde oxidase, xanthine oxidase and aldehyde dehydrogenase activities in the oxidation of vanillin, isovanillin and protocatechuic aldehyde with freshly prepared liver slices. METHODS Vani...

A lag phase in the spectrophotometric assay progress curve of aldehyde oxidation by HL-ADH was observed and characterised. The aldehyde oxidation and aldehyde dismutation reactions were shown to be related, and a mechanism to explain net aldehyde oxidation was proposed. The spectrophotometric assay was shown to be unsuitable for measurement of kinetic parameters for aldehyde oxidation by HL-ADH...