The metabolism of the anti-tubercular drug, thiacetazone (TAZ) by human FMOs in vitro and the disposition of TAZ in vivo in mice were studied. Reverse phase chromatography confirmed TAZ to be a substrate for human FMO1, FMO2.1 and FMO3 with the formation of TAZ-sulphinic acid and TAZ-carbodiimide via a TAZsulphenic acid intermediate. The products are the same as those formed by the Mycobacteriu...

Previously, we have provided evidence that cytochromes P450 (P450s) and flavin-containing monooxygenases (FMOs) are involved in the oxidation of S-(1,2,2-trichlorovinyl)-L-cysteine (TCVC) in rabbit liver microsomes to yield the reactive metabolite TCVC sulfoxide (TCVCS). Because TCVC is a known nephrotoxic metabolite of tetrachloroethylene, the nephrotoxic potential of TCVCS in rats and TCVCS f...

In this study, a series of thiophenyl-chalcones derivatives was synthesized and their DPPH ABTS activities were evaluated. All exhibited high antioxidant activity. Among them, 4e ((E)-5-(3-(4-(chlorosulfonyl)-3-hydroxyphenyl)-3-oxoprop-1-en-1-yl)thiophene-2-sulfonyl chloride) have higher activity (IC50 = 13.12 μM) than quercetin 15.49 μM), well-known as agent used standard. The structure-activi...

3-chloro-2-{(2Z)-2-[1-(4-methoxyphenyl)ethylidene]hydrazinyl}pyridine (HL) was prepared and its structure elucidated by LC/MS-MS, 1H 13C-NMR, UV-Vis, elemental analysis, FT-Raman FT-IR. All theoretical calculations optimized geometry were obtained from the 6-31G(d,p) basis set calculations. Calculated scaled data of molecule compared with observed FT-IR spectroscopic data. The chemical shifts H...