Biomedical subjects
Publications and source records attributed to G Giovanninetti.
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.
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 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.
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.
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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).
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.
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.
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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.
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.
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