Category: benzothiophene

Steele, T H published the artcileRenal handling of urate: application to the action of tienilic acid., Formula: C13H8Cl2O4S, the main research area is .

The renal handling of urate is complex, involving its filtration by glomeruli, partial tubular reabsorption, tubular secretion and also the reabsorption of a portion of the secreted urate. Studies employing tienilic acid, both acutely and chronically, have suggested that this compound exerts its uricosuric action and decreases the plasma urate by inhibiting renal urate reabsorption. The magnitude of the natriuretic and uricosuric actions of tienilic acid are correlated with the concentration of drug in the urine. Crystal equilibration studies have suggested that tienilic acid should not predispose to crystalluria with either uric acid or monosodium urate.

Postgraduate medical journal published new progress in MEDLINE about 40180-04-9, 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, Formula: C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Zacharias, F published the artcileTienilic acid in hypertension with hyperuricaemia., COA of Formula: C13H8Cl2O4S, the main research area is .

The biochemical and haematological changes seen with tienilic acid in comparison with other diuretics are discussed. Tienilic acid has a profound uricosuric effect which is maintained after 24 weeks of treatment. In the short term serum uric acid was usually lower on tienilic alone than on bendrofluazide and allopurinol.

Postgraduate medical journal published new progress in MEDLINE about 40180-04-9, 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, COA of Formula: C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Yü, T published the artcileEffects of diuretics on urate and calcium excretion., SDS of cas: 40180-04-9, the main research area is .

Forty-nine patients with gout, many with hypertension and/or renal calculi, were given hydrochlorothiazide, furosemide, or ticrynafen. Diuresis and increased clearances of sodium (Na), potassium (K), chloride (Cl), and calcium (Ca) occurred after a single dose of hydrochlorothiazide, 100 mg, or furosemide, 40 mg, orally. There was very slight change in urate and phosphorus clearances. With prolonged use of hydrochloride or furosemide, diuresis and increased electrolyte excretion disappeared. Urate and Ca excretion fell with hydrochlorothiazide. With long-term use of furosemide, urate excretion was suppressed, but Ca excretion was sustained. Ticrynafen produced diuresis and increased clearances of Na, K, and Cl. Calcium excretion was increased after a single dose and minimally decreased after long-term use. Most striking was the severe and rather sustained uricosuria. Though ticrynafen is an effective uricosuric, natriuretic, and antihypertensive agent, its hepatotoxicity and nephrotoxicity mitigate against its clinical use.

Archives of internal medicine published new progress in MEDLINE about 40180-04-9, 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, SDS of cas: 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Dayan, J. published the artcileStudy of the mutagenic activity of 6 hepatotoxic pharmaceutical drugs in the Salmonella typhimurium microsome test, and the HGPRT and sodium-potassium ATPase system in cultured mammalian cells, SDS of cas: 40180-04-9, the main research area is hepatotoxic drug mutagenicity.

Several pharmaceutical drugs show strong hepatotoxicity during therapeutic use: aminophenazone  [58-15-1], clofibrate  [637-07-0], nifuroxazide  [965-52-6], oxamniquine  [21738-42-1], perhexiline maleate  [6724-53-4], and tienilic acid  [40180-04-9]. Their mutagenicity was assessed in the Ames test on 6 strains of S. typhimurium, and in V79 Chinese hamster lung cells with a rat-hepatocyte-mediated metabolic activation system and the hypoxanthine-guanine phosphoribosyl transferase test and the Na+/K+ ATPase assay. Nifuroxazide was pos. in the Ames test in 2 Salmonella strains (TA100 and TA100 Frl). In the hepatocyte-mediated mammalian V79 cell system, nifuroxazide, clofibrate, and aminophenazone were neg. Oxamniquine and tienilic acid were pos. with and without metabolic activation in tests for ouabain and 6-thioguanine resistance. Perhexiline maleate was neg. for the direct induction of 6-thioguanine resistance without metabolic activation, and pos. after metabolization mediated by primary rat hepatocytes. These results suggest the need for some caution in the use of some pharmaceutical drugs because of hepatotoxicity and because 3 out of 6 drugs were shown to be slightly mutagenic in mammalian cells.

Mutation Research, Genetic Toxicology Testing published new progress about Liver. 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, SDS of cas: 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Ahokas, J. T. published the artcileInhibition of soluble glutathione S-transferase by diuretic drugs, Formula: C13H8Cl2O4S, the main research area is diuretic liver glutathione transferase inhibition; toxicity diuretic glutathione transferase.

Among several high-ceiling diuretics (bumetanide  [28395-03-1], ethacrynic acid  [58-54-8], furosemide  [54-31-9], indacrynic acid  [56049-88-8], and tienilic acid  [40180-04-9]) only ethacrynic acid was conjugated in vitro to GSH in rat liver cytosol. Ethacrynic, indacrynic, and tienilic acids were all potent inhibitors of glutathione S-aryltransferase  [50812-37-8] in the same preparation; glutathione S-alkyltransferase  [50812-37-8] and glutathione S-epoxide transferase  [50812-37-8] activities were also inhibited by these diuretics, but to a lesser extent. The most potent enzyme inhibitors are related in structure to ethacrynic acid. These observations are discussed with respect to the effect this enzyme inhibition may have on the toxicity of diuretics as well as the toxicity of other coadministered drugs which are also detoxified by the glutathione S-transferase  [50812-37-8] pathway.

Biochemical Pharmacology published new progress about Liver. 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, Formula: C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Zou, Tingting published the artcileFlavour precursor peptide from an enzymatic beef hydrolysate Maillard reaction-II: Mechanism of the synthesis of flavour compounds from a sulphur-containing peptide through a Maillard reaction, Application of 3-Acetylthiophene, the main research area is beef hydrolyzate Maillard reaction product dimethylthiazole isobutylpyrazine.

This study aims to investigate the Maillard reaction products (MRPs) generated between enzymic beef hydrolyzated sulfur-containing oligopeptides and xylose subjected to heat treatment. The priority of the meat aroma contribution is Cys-Gly-Val > GSH > Leu-Cys, whereas Val-Met is relatively Maillard inert. Two peptide-specific aroma compounds, namely, 2-Isobutylpyrazine and 4-butyl-2,5-dimethylthiazole, were produced in a Leu-Cys Maillard reaction system at pH 5.5, showing that the dipeptides with Leu in the N-terminus exhibited high Maillard reactivity. The carbon source and generation pathway of the aroma-active compounds were demonstrated by carbohydrate module labeling (CAMOLA). A new pyrazine generation pathway with xylose-contributed C2 was proposed using this method specifically. Ultra-performance liquid chromatog.-electrospray ionization/quadrupole-time-of-flight tandem mass spectrometry (UPLC-ESI-Q-TOF MS/MS) was then used to analyze the peptide-specific MRPs to reveal the peptide cleavage, cyclization, and crosslinking with other reactants and intermediates. The main results of this study include that crosslinking between reactants and their intermediates largely occurred in a peptide-specific Maillard reaction; its oligopeptide-specific MRPs were first demonstrated; and the crosslinking products from cyclopeptides and two xyloses and/or their fragments were observed for the first time.

LWT–Food Science and Technology published new progress about Beef. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Application of 3-Acetylthiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Fehring, Susan I. published the artcileEffect of the glutathione S-transferase inhibitor, tienilic acid, on biliary excretion of sulfobromophthalein, Product Details of C13H8Cl2O4S, the main research area is tienilate interaction sulfobromophthalein biliary excretion; glutathione transferase inhibitor sulfobromophthalein biliary excretion.

Tienilic acid, a phenoxyacetic acid diuretic, reduces the amount of total sulfobromophthalein (BSP) excretion in the isolated perfused rat liver (IPRL). This reduction was primarily by reduction in excretion of conjugated BSP, with excretion of unchanged BSP being relatively unaffected. TA also reduces the amount of conjugated BSP formed in vitro, indicating that its effect in the IPRL may be by means of inhibiting the glutathione S-transferase enzymes involved in the formation of the conjugate. It would appear that a reduction in the biliary excretion of BSP cannot be taken to be an indication of reduced liver function in a general sense.

Chemico-Biological Interactions published new progress about Bile. 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, Product Details of C13H8Cl2O4S.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Gibson, T. published the artcileTienilic acid in the treatment of gout and hypertension, Recommanded Product: 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is tienilic acid gout hypertension; health hazard tienilic acid.

Tienilic acid (I) [40180-04-9] (125 mg, twice daily) was given to patients with hypertension and gouty arthritis. In hypertensive patients, the supine and standing diastolic values declined progressively from 101 to 92 and 102 to 94 mm/Hg resp., over a period of 4 wk. There was a significant decrease in serum uric acid and K. I decreased hyperuricemic levels in gouty patients by 50%. Precipitation of acute gout by I probably reflects its profound effect on blood uric acid levels.

Advances in Experimental Medicine and Biology published new progress about Gout. 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

Shinosaki, Toshihiro published the artcileStop-flow studies on tubular transport of uric acid in rats, Synthetic Route of 40180-04-9, the main research area is kidney tubule urate transport uricosuric.

A stop-flow technique using pyrazinoic acid (PZO)-treated and -untreated rats was devised to evaluate drug effects on bi-directional transport of uric acid in the tubules. Constant venous infusion of test drugs to PZO-untreated rats was used to estimate their inhibitory effects on urate secretion, while their inhibitory effects on urate reabsorption was studied by i.v. administration as a bolus to PZO-treated rats. Probenecid, tienilic acid and R(+)-enantiomer of S-8666, which is the uricosuric component of a new uricosuric diuretic, decreased the (Tua/Pua)/(Tin-Pin) value in the distal and proximal tubules by inhibiting urate secretion in PZO-untreated rats. On the other hand, all of these drugs increased the (Tua/Pua)/(Tin/Pin) value in the tubules in PZO-treated rats, which suggested that they also inhibited the reabsorptive flux of urate. This stop-flow technique in rat kidney showed the possibilities of bi-directional inhibition by these drugs of urate transport in the tubules.

Advances in Experimental Medicine and Biology published new progress about Gout. 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, Synthetic Route of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Kahela, Paavo published the artcilePolymorphism of tienilic acid, Safety of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is polymorphism tienilic acid.

One amorphous and 3 crystalline forms of tienilic acid (I) [40180-04-9] were characterized by using IR spectroscopy and X-ray diffraction. Form A is stable at room temperature, while forms B and C and the amorphous form are metastable. Form B changes to form A near the m.p. and the amorphous form into form C at 120°. Further, during mech. grinding, the mixed form containing forms A and B changes to form A and the amorphous form into form C.

Acta Pharmaceutica Fennica published new progress about polymorphism tienilic acid. 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, Safety of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem