[Pyrrolidone and piperidone derivatives with antihistaminic and antianaphylactic activities. Synthesis and pharmacological study]. / Derivati pirrolidonici e piperidonici ad attivita' antiistaminica ed antianafilattica. Sintesi e studio farmacologico.

The preparation of several derivatives to oxatomide (A), with the benzimidazolinone moiety replaced by another heterocyclic residue is described. In some cases changes to the basic chain of (A) were also considered. All the new compounds were evaluated as antihistaminics (H1) and antianaphylactics. The derivatives where the heterocyclic moiety was an unsubstituted or phenylsubstituted 2-pyrrolidone or 2-piperidone residue showed antihistaminic and antianaphylactic activities similar to those of oxatomide while modification of the basic side chain with elimination of the benzhydryl group, gave a complete loss of activity. The pharmacological screening was completed by the evaluation of the barbiturate induced sleep prolongation and of acute toxicity.

[Methionine derivatives with liver protecting activity]. / Derivati della metionina ad attività epatoprotettrice.

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).

[Heterocyclic compounds with potential anti-inflammatory activity containing a 4-aminophenylalkanoic acid residue. V. Derivatives of 2,4-dihydro-3H-pyrazole-3-one]. / Composti eterociclici a potenziale attività antiinfiammatoria contenenti il residuo di un acido 4-amminofenilalcanoico. Nota V. Derivati del 2,4-diidro-3H-pirazol-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.

[Derivatives of 4-phenylcyclohexylethylamine with antidepressive activity]. / Derivati della 4-fenilcicloesiletilammina ad attività antidepressiva.

Several new derivatives of trans-1-(4-phenylcyclohexyl)-ethylamine (M.G. 6669) have been synthesized with various substituents at the alpha-carbon and/or at the amine nitrogen atom. All compounds were evaluated for a potential antidepressant activity taking M.G. 6669 as reference. They turned out to be less active than the reference substance. Pharmacological evaluation of M.G. 6669 itself was broadened during this work. The good antidepressant properties of this compound were confirmed, accompanied however by some toxic phenomena.