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Biomedical subjects

G Giovanninetti

Publications and source records attributed to G Giovanninetti.

At least 37 records · Page 2Linked to original sources
PubMed1981

Antiviral compounds. XVII - Synthesis and in vitro antiviral activity of 1-substituted 2-chloro- and 2-methoxyindole-3-carboxaldehyde thiosemicarbazones.

A series of indole-3-carboxaldehyde thiosemicarbazones with substituent variations at the 1 and 2 positions were prepared and evaluated for in vitro antiviral activity against vaccinia virus strain IHD and parainfluenza virus type 3, HA-I/CR-8 strain. The inhibitory activity of most compounds was restricted to the vaccinia virus, only compounds (III e) and (III f) being effective against both viruses. Structure-activity relationship are discussed.

Antiviral Agents↗
PubMed1981

[Preparation and beta adrenolytic activity of some derivatives of naphthol-[2,1-b]furan].

Some 1-(naphtho[2,1-b]furan-2-yl)-2-(t-butylamino)ethanols were synthesized for possible beta-adrenergic receptor blockade. The compounds may be considered to be derived from naphthyloxypropanolamines, the side chain of which is partially included in a furan ring. The pharmacological profile of 1-(naphtho[2,1-b]furan-2-yl)-2-(t-butylamine)ethanol (I b) is quite similar to that of propranolol without cardiac depressant properties.

Adrenergic beta-Antagonists↗
PubMed1981

[Substances with antiviral. XVI. Thiosemicarbazones containing benzofuran and 1H-indene moieties].

A few hydrazones with benzofuran and 1H-indene moieties were synthesized and screened in vitro against vaccinia virus strain IHD, parainfluenza type 3 virus strain HA-1/CR-8, and the MP mutant of herpes simplex virus type 1 [HSV-1 (MP)]. Only the thiosemicarbazones were active. The thiosemicarbazone of 3-chloro-2-formyl-1H-indene inhibited vaccinia virus to a greater extent than methisazone, used as reference standard. Furthermore, this compound was active also against parainfluenza and herpes viruses.

Antiviral Agents↗
PubMed1981

[Substances with antiviral activity. XIX. Amidinohydrazones of formylesters and formylthioesters with aromatic N-heterocyclic substrates].

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.

Antiviral Agents↗
PubMed1981

[Substances with antiviral activity. XX. Thiosemicarbazones of 1-substituted 3-formyl-2-ethoxycarbonyl(carboxy)indoles].

A series of 3-formyl-2-ethoxycarbonyl(carboxy)indole thiosemicarbazones 1-substituted were synthesized and evaluated for in vitro antiviral activity against vaccinia virus strain IHD. The thiosemicarbazone of 1-(m-chlorobenzoyl)-3-formyl-2-ethoxycarbonylindole [(II g); Table II] was the most active compound. Some structure activity relationships are discussed.

Antiviral Agents↗
PubMed1980

[Substances with antiviral activity. XV. Preparation and antiherpes activity of alkyl- and acylamino-dihalogenated pyrimidines and pyridines].

Some dihalo-amino-pyrimidines and -pyridines were alkylated and acylated at the amino group. The resulting twenty-four compounds were then tested for their action on Herpes simplex virus infection in human HEp-2 cell cultures. Five compounds were active and 2-benzamido-3,5-dichloropyridine [(III B); Table I] showed the highest antiviral activity.

Antiviral Agents↗
PubMed1980

[Substances with antiviral activity. XIII. Synthesis and in vitro activity of thiosemicarbazones of 1-benzoyl- and 1-benzyl-2-chloro-3-formylindoles].

A series of 1-benzoyl- and 1-benzyl-2-chloro-3-formylindole thiosemicarbazones was synthesized and investigated for antiviral activity against vaccinia virus IHD strain and parainfluenza virus type 3, HA-I/CR-8 strain. The results confirmed the previously observed high activity against vaccinia virus of m-substituted benzoyl derivatives. On the contrary, the analogous benzyl derivatives showed marginal activity; the compound (V c), however, was the most active against the parainfluenza virus.

Antiviral Agents↗
PubMed1980

[Effect on lipidemia in the rat of bis-homoanalogs of adenine nucleosides].

The hypolipidemic activity of a series of adenine nucleosides bis-homoanalogues was evaluated in the rat and compared with that of the sodium salt of erythadenine, used as reference standard. Some compounds were more effective in lowering serum cholesterol than erythadenine, but all showed a reduced effect on serum triglyceride content.

Adenine Nucleotides↗
PubMed1979

[Homoanalogues of pyrimidine nucleosides. XII. 3,6-anhydro-1,2-bis-desoxy-1-(pyrimidin- and 5-halopyrimidin-1-yl)-D-arabinohexitols; 3,6-anhydro-1-desoxy-1(5-halopyrimidin-1-yl)-D-glucitols].

Lithium aluminium hydride reduction of 3,6-anhydro-1-o-benzoyl-4,5-o-isopropylidene-2-o-p-tolylsulfonyl-D-mannitol (II) gives with 74% yield 3,6-anhydro-2-deoxy-4,5-o-isopropylidene-D-arabino-hexitol (III). This compound is used as its corresponding 1-o-p-toluene-sulfonate (IV) for the N-1 alkylation of uracil, 5-fluorouracil, thymine and N-acetylcytosine. Acidic cleavage of the acetal protecting group gives the expected bis-homoanalogues of the pyrimidine- and halopyrimidine-nucleosides (V-VIII) which are characterized mainly through their mass spectra and U.V. absorption. 3,6-Anhydro-1,2-dideoxy-1-(5-bromo- and 5-iodouracil-1-yl)-D-arabino-hexitols (XIII, XIV), 3,6-anhydro-1-deoxy-1-(5-bromo- and 5-iodouracil-1-yl)-D-glucitols (XV, XVI) are similarly prepared by direct halogenation of the corresponding uracil derivatives. Results of cytotoxic, cytostatic and antiviral tests are described.

Animals↗
PubMed1978

[Research on substances with antiviral activity. VIII. Benzindanoncarboxylic acids].

New derivatives (esters, amides, nitriles, amidines, thiosemicarbazones and guanylhydrazones) of 1H-benz[e]indene-2,3-dihydro-5-methyl-1-oxo-3-carboxylic acid and 1H-benz[e]indene-2,3-dihydro-7-methyl-3-oxo-1-carboxylic acid were prepared and tested for antiviral activities in vitro against vaccinia virus, HID stock and parainfluenza type 3 virus, HA-I/CR-8 stock. Four compounds (II g), (II i), (III b), (III g), showed weak activity in vitro against vaccinia virus.

Antiviral Agents↗
PubMed1978

[Substances having antiviral activity. IX. Synthesis and antiviral activity of 1-acyl-2-halo-3-formylindole thiosemicarbazones].

Some thiosemicarbazones of 1-acyl-2-chloro-3-formylindoles were synthesized and investigated for antiviral activity against vaccinia virus, HID stock and parainfluenza virus type 3 HA-I/CR-8 stock. Evidence of antiviral activity was found only against vaccinia virus, and was particular significant with the m-substituted 1-benzoyl-2-chloro-3-formylindoles. The first results of 2-substitution of chlorine by bromine in the indole skeleton, are reported.

Antiviral Agents↗
PubMed1977

[Studies of substances with antiviral activity. VI. Activity on Herpes simplex virus of bis-homoanalogs of nucleosides and of hydrazone derivatives of various aromatic substrates].

Derivatives of different chemical structures, namely hydrazones of aromatic compounds and bis-homoanalogues of pyrimidine and purine nucleosides, have been investigated for inhibiting activity on Herpes simplex virus infection of human HEp-2 cell cultures. Some thiosemicarbazones, nucleoside analogues and guanylhydrazones proved active [compounds (I), (II b), (II c), (III), (IV a), (IV b), (V a), (V b); Fig. 1]. An increase in the number of guanylhydrazone chains linked to a fluorene structure [from 1 to 3: compounds (II a), (II b) and (II c)] increased the "activity index" (i.e., toxic versus active concentrations: Table II). Further in vitro investigations have been carried out on bis-guanylhydrazone of 1-phenyl-2-chloro-3,7-diformylindole (I) and it was found that its activity is of the order of 1 microgram per ml (Fig. 3). The compound completely blocks low multiplicity infections while it only blocks cytopathogenicity, not viral replication, in high multiplicity infections.

Antiviral Agents↗
PubMed1977

[Research on substances with antiviral activity. VII. Activity and lipophilic of property N-alkyl-2-chloro-3-formylindole thiosemicarbazone].

Thiosemicarbazones of N-alkyl-2-chloroindole-3-carboxaldehydes were synthesized and investigated for antiviral activity against RNA virus (parainfluenza type 3, HA-I/CR-8 stock) and DNA virus (vaccinia virus, HID stock). The effect of lipophilicity on the activity against vaccinia virus was considered. Relative lipophilicities were measured by a reversed phase thin-layer chromatographic technique. The most active compound N-isopropyl-2-chloroindole-3-carboxaldehyde thiosemicarbazone appeared comparable for its activity to methisazone.

Antiviral Agents↗