Antibacterial activity and pharmacokinetics in mice of two new derivatives of norfloxacin.
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Biomedical subjects
Publications and source records attributed to F Dubini.
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alpha-Mercaptopropionylglycine (tiopronin, Mucolysin), a drug endowed with an interesting mucolytic activity, was tested for mutagenicity by means of the following in vitro and in vivo tests: mutagenesis on S. typhimurium with and without metabolic activation, genetic mutation on S. pombe P1 with and without metabolic activation, gene conversion on S. cerevisiae D4 with and without metabolic activation, urinary assay in the mouse with S. cerevisiae D4, host mediated assay in the mouse with S. cerevisiae D4 and micronucleus test in the mouse. On the basis of the results obtained tiopronin proved to be free of mutagenic activity.
The synthesis of a new class of imidazole derivatives with the structure of 1-[2-(2,4-dichlorophenyl)-2-tert.amino]ethylimidazoles is described. Preliminary data on their antimicrobial activity are reported.
The in-vitro antibacterial activity of a fluorinated analogue of thiamphenicol, Sch 25393, has been evaluated in comparison with chloramphenicol and thiamphenicol. The substitution of an hydroxyl group at position 3 and of two atoms of chlorine with fluorine in the acyl side-chain improves remarkably the antibacterial activity of the compound against strains resistant to chloramphenicol and thiamphenicol because of the production of acetyltransferases, but not against strains resistant because of non-enzymatic mechanisms of resistance. Although itself resistant to the enzymatic inactivation, Sch 25393 is unable to inhibit the acetylation of chloramphenicol and thiamphenicol.
The focal microbial flora composition has been studied in patients affected by irritable bowel syndrome. The statistical analysis of the results showed a decrease of coliforms, lactobacilli and, to a lesser extent, bifidobacteria, as compared to control healthy individuals. Hypotheses on the cause of these modifications and their role in the maintenance and severity of the disease are discussed.
The transmethylating activity of ATCA was directly evaluated by administering ATCA 14C to a group of rats. The radioactivity associated with the labile methyl group was recovered in microsomal phospholipids, and in particular in the phosphatidylethanolamine and phosphatidylcholine fractions. These biochemical data on the transmethylating activity of the drug confirm a previous indirect demonstration of the protective activity of ATCA in experimental intoxications and elucidate its mechanisms.
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Chloroimipramine in vitro on human lymphocytes stimulated by phytohaemoagglutinin at concentrations from 1 to 10 g/ml leads to mitotic block. Treatment of normal or suprarenalectomized rats with high doses of the drug administered orally leads to a reduction in the weight of the thymus. The hypothesis that chloroimipramine possibly plays a part in immunitary processes is put forward.
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