Heterocyclic Building Blocks-Benzothiophene

Murray, T G published the artcileTicrynafen in anephric patients: effects on uric acid and pharmacokinetics., Safety of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

Ticrynafen was given to 6 anephric patients undergoing maintenance hemodialysis. Ticrynafen was given daily for the 3 days between hemodialyses. Ticrynafen had no effect on the interdialysis rise in serum uric acid levels. Ticrynafen did not accumulate in serum, but levels of metabolites continued to rise over the 3 days. Hemodialysis (5 hr) reduced levels of ticrynafen by 38% but had less effect on metabolite levels. There was no effect on serum cholesterol or triglycerides.

Clinical pharmacology and therapeutics 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, Safety of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Homberg, J C published the artcileA new anti-liver-kidney microsome antibody (anti-LKM2) in tienilic acid-induced hepatitis., Synthetic Route of 40180-04-9, the main research area is .

The sera of 131 patients with anti-liver-kidney microsome antibodies (anti-LKM) detected between 1973 and 1979 in two different laboratories were re-examined. (1) Eighty-six anti-LKM corresponded to the description given by Rizzetto, Swana & Doniach (1973), with a pattern of fluorescence predominating on the 3rd portion of the proximal tubules (P3). This group comprised 45 cases of idiopathic chronic hepatitis or idiopathic cirrhosis and one case of halothane-induced hepatitis. (2) Forty-five anti-LKM gave a different pattern on male mouse liver and male rat kidney: (a) fluorescence was greater on centrolobular than on periportal hepatocytes; (b) the first and second portions of proximal tubules (P1 and P2) predominated over P3; (c) P1 fluorescence was equally intense as P2 and (d) P3 cells were heterogeneous with one cell out of 20 more positive than the rest. Absorption tests confirmed that the corresponding antigen was also present in the liver microsomal fraction. A retrospective clinical study discovered tienilic acid-induced hepatitis in all cases. We suggest naming this new antibody ‘anti-LKM2’.

Clinical and experimental immunology 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, Synthetic Route of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Wong, C M published the artcileComparison of the metabolic and antihypertensive properties of tienilic acid and hydrochlorothiazide., Computed Properties of 40180-04-9, the main research area is .

Tienilic acid (2,3-dichloro-4-(2-thienylcarbonyl) phenoxyacetic acid) is a new diuretic with uricosuric properties. Eighteen patients, aged between 37 and 67 years, with moderate arterial hypertension underwent a double-blind, within-patient, crossover study to compare the effects of tienilic acid (TNCF) and hydrochlorothiazide (HCTZ) on blood pressure, renal function, serum levels of uric acid and electrolytes, and liver function. Blood pressure was lowered similarly by TNCF and HCTZ. The prime advantage of TCNF over HCTZ was its profound hypouricaemic effect. Despite the possibility of hepatotoxicity of TNCF, it may still have a place in the treatment of hypertensive hyperuricaemic patients when the mechanism of hepatotoxicity of TNCF is elucidated.

The Medical journal of Australia 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, Computed Properties of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Reardon, J A published the artcileControlled inpatient study of tienilic acid in treatment of gout and hypertension., Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

Under inpatient controlled conditions 4 patients with gout and hypertension were treated with varying doses of tienilic acid, a new uricosuric diuretic. Plasma urate levels were reduced by an average of 50% in association with significantly increased urinary urate excretion. A twice-daily regimen was considerably more effective than a single morning dosage in reduction of plasma urate, though both regimens were equally effective in antihypertensive potency. The single daily regimen produced greater diurnal fluctuations in plasma urate and was more frequently associated with the development of acute gout attacks.

Annals of the rheumatic diseases 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, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Gibson, T published the artcileTienilic acid: a single treatment for hyperuricaemia and hypertension?, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid, the main research area is .

Tienilic acid is a drug with established uricosuric and hypotensive properties. We have examined its potential role as a single treatment for hyperuricaemia and hypertension, 2 disorders which are commonly associated. In 17 subjects with gout, blood uric acid levels were reduced by approximately 50%. Eleven of these patients also had hypertension which was improved by tienilic acid. However, a statistically significant effect was observed only with standing diastolic blood pressure. Side effects included acute episodes of gout in 4 patients and transient loin pain and dysuria in 1 patient. The precipitation of gouty arthritis is an acknowledged risk of all potent hypouricaemic drugs. The hazard of urate deposition in the renal tract implicit in the history of loin pain is a more serious complication. Thus, it would appear that tienilic acid is a potentially valuable drug which may have a special role in patients with hyperuricaemia and hypertension. Further study is necessary to determine how it may be best administered without the risk of renal damage.

Annals of the rheumatic diseases 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, Application of 2-(2,3-Dichloro-4-(thiophene-2-carbonyl)phenoxy)acetic acid.

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

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

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

Freis, E D published the artcileDouble-blind assessment of tienilic acid in essential hypertension., Application In Synthesis of 40180-04-9, the main research area is .

The antihypertensive effectiveness of tienilic acid in doses of 250 mg once and twice daily was compared to hydrochlorothiazide 50 mg once and twice per day in a randomized double-blind trial lasting six weeks. Blood pressure fell significantly and to a similar extent with the larger dose of both drugs. This was accompanied by a slight decrease in body weight and serum potassium concentration and a slight increase in serum creatinine and blood urea nitrogen. The magnitude of these changes was similar with both drugs. Unlike hydrochlorothiazide, however, the administration of tienilic acid was associated with a marked drop in the concentration of serum uric acid. No disturbing side effects or evidence of serious toxicity were noted during treatment with the new drug.

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, Application In Synthesis of 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Dubb, J W published the artcileTienilic acid: pharmacokinetics, salicylate interaction and creatinine secretion studies., HPLC of Formula: 40180-04-9, the main research area is .

Tienilic acid is a diuretic-uricosuric compound whose natriuretic site of action is in the cortical diluting segment of the distal nephron. Oral doses of 250 mg given to normal human volunteers provided peak blood levels of 10–11 micrograms/ml at 3–4 hours after administration. Approximately 40% of the dose was recovered in 24 hours, 30% as the parent compound and 10% as the alcohol and diacid metabolites. A 650 mg dose of acetylsalicylic acid significantly decreased the uricosuric effect of tienilic acid by inhibiting uric acid secretion. Urine pH fell significantly with tienilic acid administration. Tienilic acid inhibited salicylate excretion by either competition for tubular secretion or by increasing passive, pH dependent reabsorption. In normal subjects given a creatinine load, tienilic acid did not inhibit creatinine secretion.

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, HPLC of Formula: 40180-04-9.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem