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Biomedical subjects

L Garuti

Publications and source records attributed to L Garuti.

46 records · Page 3Linked to original sources

[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↗

[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↗

[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↗

[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↗

[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↗

[Homoanalogs of aldofuranosylnucleosides. XI. 3,6-Anhydro-1-deoxy-1-(5-halogenouracil-1-yl)-D-mannitol].

3,6-Anhydro-1-deoxy-1-(5-bromouracil-1-yl)-D-mannitol (II) and 3,6-anhydro-1-deoxy-1-(5-iodouracil-1-yl)-D-mannitol (III) were prepared by direct halogenation of the corresponding bis-homonucleosides; the 5-fluoro isomer (V) was prepared by N-alkylation of 5-fluorouracil by 2-o-acetyl-3,6-anhydro-4,5-o-isopropylidene-1-o-p-tolysulfonyl-D-mannitol in dimethylsulfoxide in the presence of potassium carbonate followed by hydrolysis of the protective groups in an acid medium. The ultraviolet spectroscopy, mass spectrometry and nuclear magnetic resonance studies of these compounds are described and the results of pharmacological tests on L 1210 leukemic cells are given.

Antineoplastic Agents↗