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Biomedical subjects

G Picciòla

Publications and source records attributed to G Picciòla.

12 recordsLinked to original sources

[Methionine derivatives with liver protecting activity].

Some methionine derivatives with the amine group acylated with an aliphatic group bearing a free, esterified or etherified thiol group in the omega position were prepared and tested for protection against CCl4, paracetamol, ethyl alcohol and ethionine intoxication. Acid (XIV) (MG 28013) (Table I) and some of its alkyl derivatives (XVIII) (MG 28228) and (XIX) (MG 28226) proved to have significant activity in these tests. A more in-depth study on MG 28226 however indicated a slight intolerance when subacute toxicity was examined (90 gg).

Acetaminophen↗

[Synthesis and pharmacologic study of new esters of naproxen with derivatives of N-oxyethylpiperazine].

The preparation of naproxen esters with N,N'-dioxyethylpiperazine and derivatives of N-oxyethylpiperazine with various substituents on the nitrogen is described. Study of analgesic-antiinflammatory properties in comparison with a reference compounds has shown that in most of the new compounds analgesic activity (phenylquinone) is preserved whereas antiinflammatory activity (carrageenin) is generally reduced. The diester with N,N'-dioxyethylpiperazine (MG 28136) proved most interesting, showing clear pharmacological activity and very low toxicity.

Animals↗

Pantetheine and pantethine esters with hypolipidemic nicotinic acid derivatives.

We prepared several esters of pantetheine and pantethine, respectively, with 3-pyridineacetic acid and with 3-(3-pyridinemethoxycarbonyl)propionic acid, and we tested these products for their capacity to lower serum non-esterified fatty acids and triglycerides in normal animals. Among the products thus tested, the tetraester of pantethine with 3-(3-pyridinemethoxycarbonyl)propionic acid (MG 28362) displayed marked hypolipidemic activity, the action being of uncommonly long duration.

Animals↗

[Heterocyclic compounds with potential anti-inflammatory activity containing a 4-aminophenylalkanoic acid residue. V. Derivatives of 2,4-dihydro-3H-pyrazole-3-one].

The synthesis and pharmacological study of some derivatives of 2,4-dihydro-3H-pyrazol-3-one of general formula (I) are described. The compound in which R = C6H5 and R' = CH3 [2-(4- carboxymethylphenyl )-4-phenyl-5-methyl-2,4- dihydropyrazol -3-one] (MG 18949) proved to have antipyretic activity equal to that of ibuprofen and aminopyrine.

Analgesics↗

[Heterocyclic compounds containing a 4-aminophenylalkanoic acid group with potential antiinflammatory activity. II. 2-Substituted morpholine derivatives].

Derivatives of 4-aminophenylalkanoic acids where the amino groups is part of a 3-morpholinone or a 2-morpholine ring, substituted in position 2 with a methyl, phenyl, 2-thienyl or (2-cyclohexyl)phenoxymethyl residue are described. Pharmacological evaluation aimed at evidencing analgesic and anti-inflammatory activity gave no noteworthy results.

Animals↗

[Heterocyclic compounds containing the residue of a 4-aminophenylalkanoic acid with potential anti-inflammatory activity. IV. Derivatives of 2-phenyl-2H-indazole].

Numerous derivatives of 2-phenyl-2H-indazole were prepared. The compounds were of general formula I: where R is an acid, neutral or basic radical and R1, R2, R3 represent various functional groups, hydrogen atom or chlorine. The compounds were examined for analgesic-antiinflammatory properties and in some cases as inhibitors of platelets aggregation. Among the compounds where R is an alkanoic acid residue, the only compound showing interesting activity was M.G. 18755 [R = CH(CH3) COOH; R1, R2, R3 = H] and its lysine salt (M.G. 18334), which in various tests showed activity greater than that of ibuprofen. The homologous butyric derivative (M.G. 18860) showed a good anti-aggregatin activity.

Animals↗

[2-(2-Thienyl)morpholines with CNS activity].

The synthesis and pharmacological investigation of 2-(2-thienyl)morpholine and some of its derivatives substituted on the nitrogen are described. The non-substituted compound showed interesting antidepressive properties with a pharmacological profile similar to that of imipramine.

5-Hydroxytryptophan↗

[Cyclohexylphenoxymorpholines with antidepressive activity].

A report is given of the synthesis and pharmacological investigation of some cyclohexylphenoxymethylmorpholines of general formula: Formula: (see text). The compound in which R = H and bearing the cyclohexyl group at the ortho position showed a pharmacological profile typical of drugs with antidepressant activity and was studied in detail in comparison with viloxazine and imipramine.

Aggression↗

Cyclohexylphenoxy amidoximes and imidazolines with antidepressive and alpha-adrenergic activity.

The effect of variation of the cycloaliphatic residue position on pharmacological activity was studied in two series of cyclohexylphenoxy derivatives (A and B). (Formula: See text) The ortho derivatives generally exhibit remarkably strong activity; (A) has an imipramine-like pharmacological profile; (B) with Y = H is more active than naphazoline and xylomethazoline as vasoconstrictor. The meta and para substituted derivatives and all (B) derivatives with R = CH3 exhibited no definite or interesting pharmacological activities.

Adrenergic alpha-Agonists↗