Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Bridged-Ring Compounds”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

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

At least 163 records · Page 9Linked to original sources
PubMed1977

Induction of the platelet release reaction by 1.3-dimethyl-5-aminoadamantane, a new adamantane derivative.

The amantadine derivative 1.3-dimethyl-5-aminoadamantane, D 145, induces in high concentrations of 2-10 mM the release reaction. Adenine nucleotides and 5-hydroxytryptamine (5-HT) are liberated to the same extent and in the same ratio as found after thrombin-induced release. The time course of release is very slow; maximal release is reached in 15-20 min. The process is temperature-dependent and dependent on energy derived from glycolysis and oxidative phosphorylation. Extracellular Ca++ does not promote the release process. D 145, in accordance with the mother-substance amantadine, inhibits 5-HT uptake non-competitively, KI = 0.15mM. In concentrations of 0.1-1 mM D 145 triggers only the liberation of 5-HT, adenine nucleotides are not liberated. The ADP induced platelet aggregation is completely inhibited after preincubation with a 1 mM solution of D 145.

Adamantane↗
PubMed1977

[Antiviral agents / 9th communication: virustatically active N-(1-adamantyl)-thiourea derivatives based on cyclic secondary amines (author's transl)].

By nucleophilic addition of pyrrolidine (2a), piperidine (2b), 3-hydroxypiperidine (2c), and 4-hydroxypiperidine (2d) on 1-adamantyl-isothiocyanate (1), the N',N'-disubstituted N-(1-adamantyl)-thiourea derivatives 3a, 3b, 3c, and 3d are accessible. Particularly 3d exhibits remarkable antiviral activity vaccinia and herpes virus.

Adamantane↗
PubMed1979

[Pharmacological study on treptilamine in man/study on tolerability (author's transl)].

N,N-Diethyl-N-(2-[alpha(tricyclo[2,2,1,0(2,6]hept-3-ylidene)-benzyloxy]-ethyl)amine hydrochloride (treptilamine) which in experiments on animals showed distinct spasmolytic effects, has been investigated first in 6 volunteers with regard to compatibility using different doses p.o. and i.v. In connection with this previous study a double blind study including placebo was performed for verification of the observed effects. In the plot study 30, 40 and 50 mg were applied orally and 10, 15 and 20 mg treptilamine were used i.v. The double blind study was designed for 20 volunteers at dosages of 40 mg p.o. and 15 mg i.v. against placebo. In the pilot study systolic blood pressure decreased significantly 5 to 15 min after i.v. application of the substance for 5 or 30 min. The range of accommodation was restricted depending on the dose used. No alteration of circulation was observed after oral application at any dose. All volunteers felt tired. A significant decrease of systolic blood pressure (15 mmHg for 10 min immediately after application) occurred after 15 mg of substance were applied i.v. in the double blind study. No effect on circulation could be seen after placebo. The range of accommodation was restricted in a significant way both after i.v. application (40%) and after oral application (30%). Two of five volunteers recorded a burning sensation in the venous wall which was followed by drowsiness. One volunteer felt increasingly tired after oral application. No influence of the substance could be seen on the clinicochemical parameters examined.

Accommodation, Ocular↗
PubMedDate not supplied

[Use of rimantadine in familial foci during an epidemic of influenza caused by A1 virus].

The therapeutic and prophylactic efficacy of rimantadine in familial foci during influenza A1 outbreaks was studied. The observations included 28 experimental foci and 26 control (altogether 146 subjects varying in ages from 4 to 71 years). The foci were selected at random (the alphabet principle). In the experimental foci the patients were treated with rimantadine given in single doses of 300 mg on the first day, 200 mg on the second, and 100 mg each on the 3rd and 4th days. The contacts were also given rimantadine, 100 mg each for 7 to 10 days. In the control foci the patients received symptomatic drugs and contacts were only observed by physicians. Rimantadine was shown to be effective therapeutically if the treatment was started on the first day of the disease. As compared with the control group, in the treated patients the temperature became normal and the main symptoms of the disease regressed within shorter periods of time. The prophylactic effect was also positive: in experimental foci repeated diseases occurred only in 3 subjects (6%) and in controls 13 subjects (30%). The prophylactic effectiveness of the drug is also indicated by a decline in the number of inapparent forms: in experimental foci 26%, in control 56%. The drug may be recommended for treatment and prevention of influenza in familial foci when the disease is caused by A1 virus.

Adamantane↗
PubMed1976

On the structure-activity relationship of antiviral substances.

The significance of the study on structure-activity relationship in the antiviral substances is considered for: 1. directed synthesis of highly active and selective antivirals; 2. elucidation of the mechanism of action of antiviral substances by revealing the chemical structures which determine the inhibition of a given step in the virus growth cycle. The basic trends in conducting directed synthesis of antiviral substances are pointed out: synthesis of new inhibitors with a broad antiviral spectrum, as well as improvement by structural modifications of known ones. The basic methodological approaches in the structure-activity studies are considered. A classification of the available antiviral synthetic substances is presented.

Anti-Bacterial Agents↗
PubMedDate not supplied

[Comparative study of the antiviral activity of rimantadine and bonafton].

The results of the study on toxicity and the antiviral activity of bonaphthone and rimantadine are presented. A high toxicity of bonaphthone for developing chick embryos was demonstrated, the maximum non-toxic dose of bonaphthone being about 10 microgram/embryo, while for rimantadine it was above 1000 microgram/embryo. In white mice, however, the toxicity of these two drugs was approximately similar. The minimal single lethal dose for mice by the oral route was 400-500 mg/kg for rimantadine and bonaphthone, by the intraperitoneal route 65 mg/kg for bonaphthone and 125 mg/kg for rimantadine. Bonaphthone had a slight prophylactic activity protecting mice inoculated with A2/Bethesda/63 influenza virus. The index of effectiveness of bonaphthone was about 40%, that of rimantadine under similar experimental conditions over 90%. Bonaphthone had no therapeutic effect. It inhibited multiplication of A2/Hong Kong/68 influenza virus in the lungs of mice inoculated with minimal doses of the virus, but was inactive in case of infection of mice with A/Port Chalmers/73 virus. Thus, the comparative study of bonaphthone and rimantadine revealed no superiority of bonaphthone.

Adamantane↗
PubMedDate not supplied

[Study of the sensitivity of different strians of the influenza A2 virus of rimantadine].

The sensitivity of different influenza A2 (H3N2) virus strains to rimantadine in ovo was studied. The reference strains of influenza virus A/Hong Kong/1/68, A/England/42/72, A/Scotland/840/74 as well as new epidemic strains isolated in the USSR and Mongolia in 1974-1975 antigenically related to influenza A/Port Chalmers/1/73 virus were found to be sensitive to rimantadine.

Adamantane↗
PubMedDate not supplied

[Therapeutic effectiveness of bonafton and rimantadine in influenza].

The therapeutic effectiveness of bonaphthone and rimantadine was studied by treatment of 439 patients with influenza between 18 and 21 years of age (bonaphthone 94, controls 105, rimantadine 120, controls 120). No therapeutic effectiveness of bonaphthone was established in the study. When rimantadine was given to the patients from the 1st day of the disease, shorter intervals of normalization of the temperature, disappearance of toxicity and catarrhal symptoms were observed than in patients treated with symptomatic drugs. During the period of rimantadine therapy the rate of findings the influenza antigen in smears from the nasal mucosa was lower, but after termination of the course of treatment the antigen was found twice as frequently as in the control group. With the positive therapeutic effect in patients treated with rimantadine, the diagnostic rise of antibody in this group was observed in a lower per cent of cases than in the control group (13 and 20%, respectively). The results of immunofluorescent and serological studies indicate a possible virus reproduction-inhibiting effect of rimantadine. This, however, requires further study. On the basis of the above observations rimantadine may be recommended for treatment of patients with influenza.

Adamantane↗