PubMed Health⌕ Search

SEARCH · PubMed Health

Results for “Spiro Compounds”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 181 records · Page 10Linked to original sources
PubMedDate not supplied

[Structural changes in erythrocyte ghosts after irradiation and the initiation of lipid oxidation detectable using 2,6-TNS and fluorescamine].

It was shown on erythrocyte ghosts that the parameters of fluorescence of 2,6-toluidine-naphthalene-sulfonate (2,6-TNS) and fluorescamine undergo similar changes after irradiation. After a dose of 100 Gy the equally effective concentrations of Fe2+ were 1-5 microM and 50-100 microM with regard to changes in the rate of fluorescence of fluorescamine and 2,6-TNS, respectively, and greater than 100 microM with regard to fluorescence anisotropy.

Animals↗
PubMed1994

Study of structure/activity relationships by multivariate statistical analysis in a series of triazaspirodecanediones with CNS activities.

The CNS activities of thirteen triazaspirodecanediones have been compared by multivariate statistical analysis. The response parameters used in this study were spontaneous motor activity, potentiation of pentobarbital effect, anticonvulsant and anxiolytic activities. Pharmacological data were analyzed using two methods: (1) a factorial correspondence analysis; (2) an automatic analysis based first on a hierarchical clustering represented by a dendrogram and second on the minimum spanning tree method. The obtained results allow to imagine the synthesis of more specific compounds.

Animals↗
PubMed1989

Inhibition of converting enzyme in the cerebrospinal fluid of rats after oral treatment with converting enzyme inhibitors.

Inhibition of brain converting enzyme (CE) has been implicated in the antihypertensive action of some CE inhibitors. However, it is still a matter of debate whether these drugs gain access to the central nervous system upon systemic administration. In this study in rats we investigated the ability of p.o. applied CE inhibitors to penetrate from blood into cerebrospinal fluid (CSF) by analyzing the inhibition of CE activity in the CSF after acute bolus and after 1 week overnight treatment with enalapril, ramipril and Hoe 288. Penetration into the CSF closely paralleled the lipid solubility of the drugs. The most lipophilic drug, Hoe 288 (10 mg/kg), inhibited CE activity in the CSF after acute (66%) and after chronic (30%) p.o. treatment. Ramipril (10 mg/kg), being less lipophilic than Hoe 288, was only effective after acute bolus administration (59% inhibition), whereas the most hydrophilic drug, enalapril (30 mg/kg), did not reduce CE activity in the CSF after either regimen. The CE inhibition in the CSF after acute p.o. treatment with ramipril and Hoe 288 was dose-dependent with threshold doses of 3 to 10 mg/kg (ramipril) and less than 1 mg/kg (Hoe 288). The presence of ramipril and Hoe 288 in the CSF was also demonstrated by the inhibitory effect of heat-inactivated CSF from CE inhibitor-treated rats on purified CE from rabbit lung. A comparison of the in vitro activities of the three prodrugs and their parent diacids against CE in plasma and in CSF and against purified CE revealed hydrolysis of the prodrugs to their parent diacids in plasma and CSF.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗
PubMed1990

[Studies on antitumor drugs: the synthesis of N',N"-dispirotripiperaziniums].

In order to search for new antitumor drugs, sixteen N',N"-dispirotripiperazine derivatives were synthesized from N',N"-dispirotripiperazinium dichloride dihydrochloride by substitution, acylation and Mannich reaction. Six compounds were selected for preliminary pharmacological test. The result showed that five compounds possess inhibitory action against carcinoma S37 in rats. The inhibitory activity of compounds VI and X was 55.0% and 41.9% respectively.

Animals↗
PubMed1995

Antitumor effect of keto-diepoxides isolated from the fungus Nattrassia mangiferae.

A novel keto-diepoxide Sch 49209 and its derivative Sch 50672, produced by the fungus Nattrassia mangiferae, inhibited tumor cell invasion through an artificial basement membrane. These compounds, at nontoxic concentrations, inhibited invasion of HT-1080 cells in a dose-dependent manner. The IC50 values for Sch 49209 and Sch 50672 were 0.75 and 8 microM, respectively, when cells were incubated with drugs for 5 h. Sch 49209 inhibited both tumor cell invasion and cell motility to the same extent under conditions that did not cause any apparent cytotoxicity. Sch 4209 and Sch 50672, however, inhibited the growth of ras-transformed cells in a semisolid medium in a 5-day culture with IC50 values of 0.6 and 2.4 microM, respectively. They also inhibited the anchorage-dependent growth of pT24 cells in vitro with IC50 values of 0.5 and 0.9 microM for Sch 40209 and Sch 50672, respectively. Using the murine lung epidermoid carcinoma M27 cells implanted SC in mice as a model, we found both Sch 49209 and Sch 50672 inhibited the growth of this tumor at doses ranging from 2 to 10 mg/kg. These compounds also decreased the formation of spontaneous lung metastasis in this model. Sch 50672 inhibited the growth of human tumor xenografts, SW620 and A431, in athymic mode mice. Our data suggest that keto-diepoxides inhibit tumor growth and metastasis and that this activity may be due, in part, to anti-invasive activity.

Animals↗