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Biomedical subjects

V Cavrini

Publications and source records attributed to V Cavrini.

118 records · Page 7Linked to original sources

[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↗

[Research on substances with antiviral activity. III. Structure of the monosubstituted derivatives of 1 H-benzo-[e] indene-1,3(2H)-dione].

The N.M.R. spectra of 1H-benz[e]indene-1,3(2H)-dione (I), 1H-benz[e]indene-2,3-dihydro-1-one (II), 7-methyl-3H-benz[e]indene-1,2-dihydro-3-one (III) and of their oximes, phenylhydrazones and 4-methylthiosemicarbazones show the preferential substitution at 3 position for monoderivatives of (I). This is very interesting in correlation with the structure-activity relationship of derivatives of (I) and (II), some of which have shown in vitro antiviral action in previous research.

Antiviral Agents↗

[Research on substances with antiviral activity. II. Derivatives of N-substituted 2-chloro-3-formylindoles].

Thiosemicarbazones and amidinohydrazones of N-substituted 2-chloroindole-3-aldehydes 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 thiosemicarbazones of 1-(o,m,p,-chlorobenzoyl)-2-chloroindole-3-aldehydes were more active than methisazone against vaccinia virus.

Amidines↗

Determination of carboxylic acid salts in pharmaceuticals by high-performance liquid chromatography after pre-column fluorogenic labelling.

2-Bromoacetyl-6-methoxynaphthalene (Br-AMN) was used as a fluorogenic labelling reagent for high-performance liquid chromatographic (HPLC) analyses of pyroglutamic acid, 4-hydroxybutyric acid and thioctic acid in pharmaceutical formulations. The reaction was carried out in aqueous medium in the presence of a cationic surfactant to obtain the direct derivatization of the salts of 4-hydroxybutyric acid and thioctic acid or in acetonitrile for pyroglutamic acid. The resulting naphthacylesters were then chromatographed under reversed-phase (C-18) conditions and detected fluorimetrically (lambda exc, 300 nm; lambda em, 460 nm). The method proved to be suitable for the sensitive and selective analysis of commercial formulations of the cited acidic drugs.

Carboxylic Acids↗

HPLC-fluorescence determination of individual free and conjugated bile acids in human serum.

A method for the quantitative analysis of unconjugated and conjugated bile acids (BA) in serum of patients with primary biliary cirrhosis (PBC) before and after therapy with antibiotic or ursodeoxycholic acid (UDCA) is described. After separation of the free, glycine and taurine conjugated (F, G and T conjugated) fractions by solid-phase extraction, the isolated T conjugates were hydrolysed enzymatically using cholyglycine hydrolase. The BA fractions were derivatized using 2-bromoacetyl-6-methoxynaphthalene (Br-AMN) and detected fluorimetrically (lambda exc = 300 nm, lambda em = 460 nm). The derivatization reaction was performed under mild conditions (10 min at 40 degrees C) in an aqueous medium in the presence of tetrakis (decyl) ammonium bromide (TDeABr). The HPLC separation was achieved using an ODS column and with a mobile phase gradient mixture of A-B, where A is water and B is acetonitrile:methanol (60:40 v/v) for elution at a flow-rate of 1.2 mL/min. The reproducibility, recovery and separation of individual BA under gradient elution conditions were satisfactory, allowing a sensitive detection of each BA in serum samples with a detection limit of about 1-2 pmol.

Amidohydrolases↗

Determination of glutathione in biological samples by high performance liquid chromatography with fluorescence detection.

A selective and sensitive high performance liquid chromatographic (HPLC) method has been developed for the determination of reduced glutathione (GSH) in biological samples (rat liver, spleen and plasma). The method involved a prechromatographic thiol derivatization with methyl 4-(6-methoxynaphthalen-2-yl)-4-oxo-2-butenoate; the reaction was rapid (5 min) under mild conditions (pH 7.5 and ambient temperature) and selective for the sulphydryl group. The thiol adducts were separated on a reversed-phase C-18 column using acetonitrile: 0.05 M triethylammonium (TEA) phosphate (pH 4) solution 32:68 (v/v) as the mobile phase. Fluorescence detection (lambda em = 450 nm; lambda exc = 310 nm) was used and the detection limit (S/N = 3) was about 0.5 pmole of the injected GSH adduct. The method was also applied to the determination of total glutathione in rat plasma after a preliminary reduction with dithiothreitol.

Animals↗

HPLC analysis of imidazole antimycotic drugs in pharmaceutical formulations.

Reversed-phase HPLC on different column packing materials (Hypersil C-18, Spherisorb-CN, Chromspher-B) is used to obtain selective separations of imidazole antimycotic drugs, such as ketoconazole, clotrimazole, tioconazole, bifonazole, isoconazole, econazole, miconazole and fenticonazole. The use of a post-column on-line photochemical reactor is shown to be useful for the enhancement of the sensitivity of the HPLC analysis with UV detection. The proposed HPLC methods are applied to the analysis of commercial dosage forms (creams) with solid-phase extraction (SPE) procedure, using a diol sorbent, being found to be a convenient technique for the sample preparation giving quantitative drug recovery.

Antifungal Agents↗