Neau, E.’s team published research in Biochemical Pharmacology in 1990-03-15 | CAS: 40180-04-9

Biochemical Pharmacology published new progress about Enzyme kinetics. 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Neau, E. published the artcileHydroxylation of the thiophene ring by hepatic monooxygenases. Evidence for 5-hydroxylation of 2-aroylthiophenes as a general metabolic pathway using a simple UV-visible assay, Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is tienilic acid hydroxylation liver monooxygenase; thiophene aryl hydroxylation liver monooxygenase.

The 5-hydroxylation of tienilic acid (I) by rat liver microsomes was measured by a new, simple method involving the detection of 5-hydroxytienilic acid (II) by UV-visible spectroscopy. This assay allowed continuous detection of this metabolite and was easily used to determine the kinetic parameters of the reaction (Vmax and Km being resp., 1 nmol product formed/mg protein/min and 14 μM for liver microsomes from phenobarbital-treated rats). This activity was dependent on NADPH and inhibited by CO, SKF 525A and metyrapone, indicating that it is dependent on cytochromes P 450. The UV-visible assay is based on intrinsic properties of 5-hydroxy-2-aroylthiophenes which exist as highly conjugated anions at physiol. pH and exhibit large ε values around 390 nm. Its application to other 2-aroylthiophenes like suprofen, 2-p-chlorobenzoylthiophene and a series of 2-aroylthiophenes with various substituents on the aroyl group showed that, in general, thiophene compounds bearing a 2-arylketo substituent appear to be hydroxylated at position 5 by rat liver microsomes. The kinetic parameters of the 5-hydroxylation of suprofen and 2-p-chlorobenzoylthiophene by liver microsomes from phenobarbital-treated rats were determined and found to be similar to those for I hydroxylation.

Biochemical Pharmacology published new progress about Enzyme kinetics. 40180-04-9 belongs to class benzothiophene, name is 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, and the molecular formula is C13H8Cl2O4S, Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem