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Biomedical subjects

D Bonazzi

Publications and source records attributed to D Bonazzi.

36 records · Page 2Linked to original sources
PubMed1980

[Compounds with antitumor activity. V. Hydrazone derivatives of 5-formylimidazo(2,1-b)thiazoles and 6-substituted 2,3-dihydro-5-formylimidazo(2,1-b)thiazoles].

The synthesis of 2,3-dihydro-5-formylimidazo[2,1-b]thiazoles with different substituents at position 6 (CH3, C6H5, Cl, Br) is reported; thiosemicarbazones and tosylhydrazones were prepared from these aldehydes and from the 2,3-unsaturated analogues: these derivatives, submitted to a preliminary test, did not show significant antileukemic activity.

Animals↗
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

Nonsteroidal antiinflammatory agents. 2. Synthesis and biological activity of 2-chloroindolecarboxylic acids.

The Vilsmeier and the Arndt-Eistert reactions have been employed for the synthesis of 1-phenyl-2-chloroindole-3-acetic acid (4). The antiinflammatory activity of 2-chloroindole-3-carboxylic acid (1), 1- methyl-2-chloroindole-3-carboxylic acid (2), 1-phenyl-2-chloroindole-3-carboxylic acid (3), and 4 was compared with the activity of indomethacin in the carrageenin rat edema. The best results are given by compounds 1 and 2 bearing H or CH3 at position 1 and COOH at position 3.

Animals↗
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↗
PubMedDate not supplied

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↗
PubMedDate not supplied

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↗
PubMedDate not supplied

New alkylating agents: butyrophenone derivatives.

The antimitotic properties associated with the bis (2-chloroethyl) amino group are well known, a number of compounds bearing this group being of therapeutic interest. The choice of a suitable supporting moiety for this group is important. Our experiments on a butyrophenone derivative, ketocaine, which possesses local anesthetic activity, showed that this drug is able to modify the oxygen consumption by tissues with prevailing anaerobic metabolism and to inhibit the mitotic activity of human lymphocytes in culture stimulated by phytohemagglutinin. These observations prompted us to prepare compounds by the general formula reported in Tables I and II. All compounds were tested in mice implanted i.p. with 10(6) Ehrlich ascites tumour cells. After 24 h the animals were treated with a single dose of the compound. The antitumor activity was correlated with: position (2, 4) and length (n = 0-2) of the chain with carbonyl group; presence (R' = H, ND2) and position (2, 4) of nitro group; monofunzional or bifunzional compound. Some of these show a potent antitumor activity.

Alkylating Agents↗