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Biomedical subjects

R Bossa

Publications and source records attributed to R Bossa.

At least 19 recordsLinked to original sources

Synthesis and analgesic activity of 1-(N-methylanilinoethyl)indoles.

The synthesis of two series of 1-(N-methylanilinoethyl)indoles is reported. The first arises from the N-alkylation of indole-3-acetic acid or its methylester, while the second was prepared by means of the Witting reaction on the appropriate aldehyde. The compounds were tested in mice (hot plate test and phenyl-p-benzoquinone induced writhing test) for their analgesic activity. None of the compounds was significantly active in the hot plate test. However, N-methylanilinoethyl 1-(N-methylanilinoethyl)-3-indolylacetate (7) was the most active one in the phenyl-p-benzoquinone induced writhing test, which indicates that 7 has a peripheral analgesic effect.

Analgesics

In vitro cytotoxic activity of aryl and heteroaryl-ONN-azoxycyanides.

Some aryl-N(O) = N-X and heteroaryl-N(O) = N-CN compounds were synthetized and tested against a culture of HeLa cells. The results obtained show that the - N(O) = N beta CN function, a new cytostatic group, is useful in the design of potential antitumoral compounds.

Antineoplastic Agents

Bactericidal and antineoplastic effect of combination of norfloxacin and adriamycin.

Norfloxacin and adriamycin were tested alone and in combination for bactericidal activity against different strains of gram-negative bacteria. The antitumoral effect of a combination of norfloxacin and adriamycin was determined in mice bearing Ehrlich ascites carcinoma and in mice bearing P 388 leukemia. No interference with the antibacterial activity of norfloxacin or with the antitumoral activity of adriamycin was observed.

Animals

Potential antitumor agents X: Synthesis and antitumor activity of two nitrogen mustard derivatives related to ketocaine.

The synthesis of two nitrogen mustard derivatives (VIII and IX) related to the well-known local anesthetic ketocaine (III) is reported. These compounds were tested in mice implanted with Ehrlich ascites tumor cells, and the antitumor activity was compared with that of two previously synthesized analogues (I and II) lacking the nitro group and with that of doxorubicin. The monofunctional compound IX was inactive, but the bifunctional compound VIII showed potent antitumor activity (%T/C greater than 254 at 20 mg/kg).

Animals

Antinociceptive effect of centrally administered cimetidine and dimaprit in the rat.

Cimetidine, an H2 receptor antagonist, administered into a lateral ventricle of the rat brain caused a significant increase in tail flick latency. Dimaprit, a specific H2 agonist, failed to counteract the analgesic effect of cimetidine. In contrast, it enhanced the effect of cimetidine and per se had marked analgesic activity. The specific opioid antagonist naloxone was without effect. Pretreatment with CaCl2 completely prevented the action of cimetidine. These findings suggest that the analgesic action of cimetidine and dimaprit is not due to specific effects on H2 receptors.

Analgesia

Interaction between doxorubicin and mitomycin C on mortality and myocardial contractility in guinea pig.

The present investigations were carried out in guinea pig to ascertain whether mitomycin C has a direct cardiotoxic effect or interacts with doxorubicin-induced cardiotoxicity. I.p. administration of mitomycin C did not modify the survival rate up to 30 days, whereas the combined administration of doxorubicin and mitomycin C significantly decreased the survival time in comparison to the doxorubicin-treated group. On isolated atria, mitomycin C did not cause significant inhibition of the contractile force or an enhancement of the doxorubicin-induced negative inotropic effect. These results do not support the possibility that mitomycin C potentiates the acute cardiotoxic effects produced by doxorubicin.

Animals