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At least 37 records · Page 2Linked to original sources
PubMed1977

Synthesis and biological activity of some derivatives of thiochroman-4-one and tetrahydrothiapyran-4-one.

A small series of pyrazoles and isoxazoles derived from thiochroman-4-one has been synthesized and characterized. The compounds were examined for their in vitro inhibitory activity against Bacillus subtilis and Pseudomonas fluorescens. Among the tested compounds the pyrazole derivative from thiochroman-4-one was found to be the most effective inhibitor of growth of B. subtilis. Extensive H NMR analysis was recorded for all compounds.

Animals↗
PubMedDate not supplied

On the role of serotonin in the pathogenesis of pulmonary hypertension induced by anorectic drugs; an experimental study in the isolated perfused rat lung, II. Fenfluramine, mazindol, mefenorex, phentermine and R 800.

1. The influence of the anorectic drugs fenfluramine, mazindol, mefenorex, phentermine and R 800, an experimental compound, on pulmonary vascular resistance has been studied in the isolated, perfused rat lung. 2. R 800 caused a strong vasoconstriction, which was not antagonized by methysergide of phentolamine; the other drugs listed did not alter vascular resistance. 3. Mazindol and phentermine significantly prolonged the vasoconstrictive effect of serotonin due to inhibition of its metabolic breakdown. 4. Although fenfluramine inhibited serotonin metabolism it also prevented the vasoconstrictive effect of serotonin, due to its ability to act as a serotonin antagonist. 5. Mefenorex did not affect pulmonary vascular resistance, either directly or indirectly via a serotoninergic mechanism.

Amphetamines↗
PubMed1977

BRL 13776: a novel antihypertensive agent with interesting monoamine depleting properties.

1. Oral doses of 10-100 mg/kg of BRL 13776 lowered the blood pressure of both deoxycorticosterone acetate (DOCA)/NaCl-treated hypertensive rats and untreated normotensive rats. 2. BRL 13776 (100 mg/kg, orally) also reduced the blood pressure of renal hypertensive cats (cellophane perinephritis model). 3. No tolerance developed to the blood-pressure lowering action of BRL 13776 when an oral daily dose of 100 mg/kg was administered repeatedly for up to 15 days to hypertensive rats and cats. 4. The fall in blood pressure to BRL 13776 in rats was associated with a reduction of tissue catecholamines. 5. The catecholamine depletion occurred in all the peripheral tissues examined but in the brain was restricted to certain regions, these being the hind-brain on single dosing and the hind-brain, hypothalamus and mid-brain on repeated dosing. Catecholamine levels in the cerebral hemispheres were not affected by either single or repeated doses of BRL 13776. 6. BRL 13776 caused some reduction of the 5-hydroxytryptamine content of the heart but not of whole brain or any brain region. 7. Neither single doses (up to 900 mg/kg orally) nor repeated doses (100-300 mg/kg orally) of BRL 13776 produced any significant behavioural effects in animals. 8. BRL 13776 is a new type of agent to display both antihypertensive and monoamine-depleting properties. The reduction of noradrenaline in certain brain regions may be a cause of the antihypertensive response but depletion in the periphery could contribute in a major or minor way. The differential action on noradrenaline in the brain together with the lack of effect on 5-hydroxytryptamine might also explain the apparent absence of behavioural effects.

Animals↗
PubMed1975

Isolation and characterization of a gamma-thiochromanone-4-thiosemicarbazone-resistant mutant of vaccinia virus.

gamma-Thiochromanone-4-thiosemicarbazone (TCT) inhibits the growth of vaccinia virus in BSCl cells by interfering with viral maturation. A mutant of the virus (TCT(R)) which is resistant to this drug was isolated. This mutant also exhibits resistance to another thiosemicarbazone related compound, isatin beta-thiosemicarbazone (IBT). There is a good correlation between the cross-resistance of the two mutants IBT(R) and TCT(R) to TCT and IBT, respectively, and the similar antipoxvirus activity of these two thiosemicarbazone-related compounds.

Benzopyrans↗
PubMed1977

Radioactive conversion products of intramuscularly injected [4-14C]formononetin including sulfates in the urine of hens.

The phytoestrogen formononetin was injected intramuscularly as [4-14C]formononetin into two adult hens. Radioactive materials in the urine for the succeeding 14 days (hen 1) or 16 days (hen 2) were fractionated on DEAE-Sephadex-25 columns by elution with a gradient of NaCl; the four major fractions thus separated were examined by solvent partition, thin-layer chromatography, and enzymic cleavage. The following seven radioactive components were identified in the urine, the average proportions of each being given in terms of percentage of total 14C recovered from the urine: [14C]formononetin (4.3%); [14C]diaidzein (11.4%); [14C]equol (6.8%); [14C]daidzein monosulfate (30.4%); [14C]equol monosulfate (5.8%); [14C]diadzein disulfate (19.8%); and [14C]equol disulfate (6.5%). Small proportions of sulfates of unidentified radioactive phenols were present. Tests for presence of glucosiduronates of 14C-labelled material gave negative results. Radioactive formononetin sulfate was not detected in the urine of either hen.

Animals↗
PubMed1975

[Derivatives of isothiochromane].

In connection with a program, the purpose of which is to aim at the synthesis of molecules containing the residual phenylethylamine in a rigid structure, the synthesis of 1-methylaminoisotiocromane (IV) starting from isotiocromane (I) is hereby described.

Benzopyrans↗
PubMedDate not supplied

[Content of ubiquinone and ubichromenol in rat liver at various levels of vitamin E saturation of the body].

Ubiquinone and ubichromenol content was studied at different levels of organism supply with vitamin E. The content of these substances in the albino rat liver with vitamin E-deficiency is shown to decrease by 16 and 23%, respectively. The intravenous administration of alpha-tocopherol to the vitamin E-deficiency rats causes a gradual 45% increase in the ubiquinone content 4h after which remains at the same level for 8 h; the ubichromenol content 2 h latter is 1.7 times as high and then it lowers gradually up to the level in the avitaminous animals.

Animals↗
PubMed1992

RP 58866 and its active enantiomer RP 62719 (terikalant): blockers of the inward rectifier K+ current acting as pure class III antiarrhythmic agents.

The present article presents an overview of the pharmacologic profile of the benzopyran derivative RP 58866, a racemic mixture, and of RP 62719 (terikalant), its active enantiomer. In normal cardiac tissues studied in vitro, both drugs dose-dependently prolonged the atrial and ventricular action potential but affected neither the upstroke of the action potential nor the diastolic potential. Patch-clamp experiments demonstrated that the prolongation of the action potential induced by the drugs is due to a specific blockade of the inward rectifier K+ current. In vivo, intravenous administration to anesthetized dogs of low doses of RP 62719 consistently induced bradycardia and prolonged the atrial, nodal, and ventricular refractory periods, but did not affect the conduction velocity. Because of these properties, RP 58866 and RP 62719 exert potent antiarrhythmic and antifibrillatory actions both at the atrial and ventricular levels in various experimental models of arrhythmia. Our results demonstrate that RP 58866 and RP 62719 are K(+)-channel blockers acting as pure class III antiarrhythmic drugs.

Action Potentials↗