Some new 1,2,3,4-tetrahydroquinoline derivatives.

Two 1,2,3,4-tetrahydoquinoline-based compounds were synthesized and evaluated for antinociceptive properties. Both compounds displayed no significant analgesic activity and at the higher dose showed no characterized CNS depressant activity.

Some new 3-methoxy-5-methyl-1,4-substituted pyrazoles.

A series of 3-methoxypyrazole derivatives was synthesized and tested as antifungal agents. The substituents were chosen on the base of their lipophylicity and for their presence in well-known antifungal drugs. The compounds displayed no significant activity in vitro.

Some new quinoline-based mono and dicarboxylic acids.

Some quinoline-based mono- and dicarboxylic acids structurally related to kynurenic acid have been synthesized and screened as antagonists of neurotransmission of NMDA, AMPA and KA excitatory amino acid receptors. Higher affinity for NMDA receptor was pointed out in the short series, but all the compounds, even those with key structural features of glutamic acid showed no significant activity.

Synthesis and antimicrobial activity of some new benzodifurans and phenanthrolines.

A short series of di-functionalized benzodifurans and phenanthrolines were synthesized for in vitro antimicrobial activity. Dicarboxaldehydes, chiefly those with a phenanthroline supporting moiety, proved to be most effective, showing significant fungal growth inhibition.

Synthesis and antimicrobial activity of some N-monosubstituted 2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamides.

A short series of N-monosubstituted (aryl, aminoacyl, dipeptidyl)-2-(2-aminothiazol-4-yl)-(Z) -2-methoxyiminoacetamides was synthesized and tested for antimicrobial activity. A few members showed a somewhat interesting inhibitory action against Cryptococcus neoformans (MIC = 150 micrograms/ml).

Synthesis and antimycotic activity of some benzyloxyimino compounds.

Some benzyloxyimio compounds, related to oxiconazole and having a 1H-indole or 1H-benzimidazole moiety, have been synthesized and tested in vitro for their antimycotic activity against Candida tropicalis and C. albicans. The most active was showed to be 0-(2,4-dichlorobenzyl)-1-benzyl-5-nitro-1H-benzimidazole-2-carboxaldehyd e oxime (MIC: 25 micrograms/ml against both microorganisms). A structural feature important for the biological activity of the series appears to be presence of a benzimidazole nucleus substituted by an electron withdrawing group.

[Preparation and analgesic activity of tetrahydroquinolines and tetrahydroisoquinolines]. / Preparazione ed attività analgesica di alcune tetraidrochinoline e tetraidroisochinoline.

A series of 1,2,3,4-tetrahydroquinolines and of 1,2,3,4-tetrahydroisoquinolines were synthesised and evaluated for analgesic activity by both hot-plate and acetic acid writhing methods in rats. Te most potent compound was 2-methyl-1,2,3,4-tetrahydro-5-quinolinol (IV i) which was shown to be 1/8 and 1/50 as active as morphine according to the employed assay. The analgesic activity was shown to be associated to a not selective action on the CNS.

[Naphthofuran derivatives with potential beta-adrenolytic activity]. / Derivati naftofuranici a possibile azione beta-adrenolitica.

1-(Naphtho[1,2-b]furan-2-yl)-2-(isopropylamino)ethanol (II) and 1-(naphtho[2,3-b]furan-2-yl)-2-(isopropylamino)ethanol (III) show low beta-adrenergic blocking activity and unlike the naphtho [2,1-b]furan derivatives (1,2) do not appear to give rise to metabolites with high beta-adrenoceptor inhibitory properties. The inclusion of the --OCH2-- moiety in an aromatic nucleus larger than the benzofuran system (bufuralol, Ro 3-3528) caused loss of the biological activity.

[Hydrazines containing 1H-indene units]. / Idrazine contenenti unità 1H-indenica.

Some derivatives of N'-(5-nitro-2-furoyl)-N2-(3-chloro-1H-indenyl-2-methylene)hydrazine (I) were synthesized and screened for in vitro antimicrobial activity. None was more active than the parent compound and the greater hydrophilic character was associated with loss of inhibitory activity against gram-negative bacteria.

[Substances with antiviral activity. XIX. Amidinohydrazones of formylesters and formylthioesters with aromatic N-heterocyclic substrates]. / Richerche su sostanze ad attività antivirale. Nota XIX--Amidinoidrazoni di formilesteri e formiltioesteri consubstrati N-eterociclici aromatici.

Some formylthioester and formylester amidinohydrazones with aromatic N-heterocyclic moieties, were synthesized and screened in vitro against the MP mutant of herpes simplex virus type 1 [HSV-1 (MP)] and parainfluenza type 3 virus, HA-1/CR-8 strain. The amidinohydrazone of 1-phenyl-4-formyl-3-(ethylthio)carbonylpyrrole (I) was the most active compound.

[Research on substances with antiviral activity. XVIII. Bis-amidinohydrazones of N-heterocyclic aromatic dialdehydes]. / Richerche su sostanze ad attività antivirale. Nota XVIII - bis-amidinoidrazoni di dialdeidi aromatiche N-eterocicliche.

Some bis-amidinohydrazones of N-heterocyclic aromatic dialdehydes were synthesised and tested in vitro against the MP mutant of the herpes simplex virus type 1 [HSV - I (MP)]. Of the compounds tested, only those with and indole substrate showed some measure of biological activity.