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Biomedical subjects

G Arcari

Publications and source records attributed to G Arcari.

At least 19 recordsLinked to original sources
PubMed1986

Bicyclic compounds with potential antiulcer and/or antisecretory activity. II. 1(or 3),4,6,7-Tetrahydro-1(3)H-pyrano[3,4-d]imidazoles and 1(or 3),4,6,7-tetrahydro-1(3)H-thiopyrano[3,4-d]imidazoles.

Owing to our current interest in synthesizing and evaluating the antiulcer and antisecretory activity of bicyclic compounds, a series of 1(or 3),4,6,7-tetrahydropyrano- and 1(or 3),4,6,7-tetrahydrothiopyrano-[3,4-d]imidazoles was synthesized and tested. The biological results were compared with those of some previously described 4,5,6,7-tetrahydroimidazo-[4,5-c]pyridine and 4,5,6,7-tetrahydrobenzimidazole derivatives.

Animals↗
PubMed1985

Bicyclic compounds with potential antiulcer and/or antisecretory activity. I. 4,5,6,7-Tetrahydrobenzimidazoles.

The remarkable antiulcer and antisecretory activity of some previously described 4,5,6,7-tetrahydroimidazo[4,5-c]pyridine derivatives prompted us to further investigate related bicyclic systems. Accordingly, a series of 5-amino- and 5-aminomethyl-4,5,6,7-tetrahydrobenzimidazoles, regiospecifically alkylated in position 1, were synthesized and tested. Only a few 1-ethyl-5-amino derivatives displayed a reasonable antiulcer activity in comparison with our former class of compounds.

Animals↗
PubMed1984

New derivatives of pyrrolo and pyrido[2,1-b] quinazoline as antiulcer agents.

A series of 3-benzylidene-1,2,3,9-tetrahydro-9-oxopyrrolo-[2,1-b] quinazolinecarboxylic acids and 6-benzylidene-6,7,8,9-tetrahydro-11-oxo-11H-pyrido[2,1-b] quinazolinecarboxylic acid was synthesized and evaluated for their antiulcer activity by the test of inhibition of restraint ulcers in the rat, and for gastric antisecretory activity using the technique of Shay. Some compounds appear potentially useful for therapeutic application.

Animals↗
PubMed1983

Antihypertensive ergolinepropionamides.

The synthesis and the antihypertensive activity in rats of a series of 6-methylergolin-8 beta-yl-propionic acid derivatives are reported. The prolactin lowering activity (nidation inhibition test) in rats and the acute toxicity in mice were also studied as a measure of the specificity and safety of the potential antihypertensive compounds. From the structure-activity considerations reported here it is clear how modifications at the C8 side chain can improve the selectivity of the antihypertensive effects, whilst introducing substituents in other positions of the ergoline skeleton afforded unfavourable results in this respect. Compound 5, namely 2(R,S)-cyano-3-(6-methylergolin-8 beta-yl)-propionamide, emerged as the most interesting antihypertensive derivative.

Animals↗
PubMed1979

[A review of pharmacological studies on nicergoline].

10-Methoxy-1,6-dimethyl-ergoline-8 beta-methanol-(5-bromonicotinate) (nicergoline, Sermion) shows a strong alpha-blocking activity both in vitro and in vivo. Various studies (dog, cat, rabbit, rat, mouse, guinea-pig) show that nicergoline affects only slightly blood pressure and heart rate and increases the blood flow in brain and hind limb without affecting the splanchnic and aortic flow in normal animals. Nicergoline does not interfere with CNS functions unless applied in high doses. It stimulates the muscle oxidative metabolism and function and lacks any emetic and hallucinogenic activity. Its acute and chronic toxicity in different animal species is very low.

Adrenergic alpha-Antagonists↗
PubMed1978

Ergoline derivatives with oral, prolonged, alpha-adrenolytic activity.

The alpha-adrenolytic activity of 1-methyl-10-methoxydihydrolysergol 2-(3,5-dimethyl)pyrrolcarboxylate (XV, formula II) is, both in vitro and parenterally, quite similar to that of dihydroergotamine. By oral route the new compound is more active, and longer lasting than dihydroergotamine.

Administration, Oral↗
PubMed1975

Ergoline derivatives. Note XIII (1) alpha-adrenergic blocking drugs.

The synthesis and the pharmacological activities of 24 analogues of the alpha-adrenergic blocking drug, nicergoline (I b), are reported. The majority of the new compounds were found to be less active than (I b): the structure-activity relationships are presented and discussed.

Adrenergic alpha-Antagonists↗