Biomedical subjects
Publications and source records attributed to M Carazzone.
The substitution of the diltiazem acetyl-group with other chemical structures greatly influences its pharmacological properties as exerted upon the perfused heart. In particular, the substitution with a nicotinic group enhances its capacity of lowering Coronary Perfusion Pressure without the usual secondary effects observable on Heart Rate and Developed Pressure.
1-(2-Hydroxyethyl)-3-hydroxyl-7-chloro-1,3-dihydro-5-(O-fluorophenyl)-2H - 1,4-benzodiazepin-2-one (doxefazepam, SAS 643, Doxans) was investigated in a series of toxicological studies. Oral LD50 values were greater than 2000 mg/kg in mice, rats and dogs, while endoperitoneal LD50 values were 746 and 544 mg/kg in the mice and rats, respectively, and greater than 1000 mg/kg in the dogs. Subacute and chronic studies in rats and dogs evidenced a transient ataxia after administration of the test compound, which was dose-dependent in the subacute experiment, and occurred only at the highest dose in the chronic studies. No pathological findings were registered at necropsy or in microscopic observations, except an increase of liver weight at the highest dosage in the chronic study in the rat. Doxefazepam did not exert any teratogenic effects in rats and rabbits. Moreover in rats it did not alter the reproductive performance. The mutagenic studies did not reveal any mutagenic potential. In the cancerogenicity study in rats doxefazepam did not show positive carcinogenic potential.
By treating at 100 degrees C 2-aminonicotinic acid with ethyl N,N-dialkylmalonamate (I) and phosphorus oxychloride N,N-dialkyl-4-chloro-1,2-dihydro-2-oxo-1,8-naphthyridine- 3-carboxamides (II) were obtained. The reaction of compounds (II) with an excess of refluxing phosphorus oxychloride afforded N,N-dialkyl-2,4-dichloro-1,8-naphthyridine-3-carboxamides (III), which in turn were treated at room temperature with excess primary amines to give a mixture of isomeric N,N-dialkyl-2-(alkylamino or cycloalkylamino)-4-chloro-1,8-naphthyridine-3-carboxamides (IV) and N,N-dialkyl-4-(alkylamino or cycloalkylamino)-2-chloro-1,8-naphthyridine-3-carboxamides (V). When this last reaction was performed at 160 degrees C, only N,N-dialkyl-2,4-bis(alkylamino or cycloalkylamino)-1,8-naphthyridine-3-carboxamides (VI) were obtained; under the same conditions (IV c) or (V c) reacted with methylamine to give isomeric 2,4-bis(alkylamino)derivatives (VII) or (VIII), respectively. Compounds (II b), (III b), (IV a,c,d), (V a,c,d) were submitted to a wide preliminary pharmacological screening. Some of them, depending on the structure, showed antihypertensive [(IV c)], anti-inflammatory [(IV c) greater than (III b)], or, in the behavioral test, anti-aggressive [(IV d) greater than (III b)] activity. Furthermore compound (III b) caused moderate inhibition of the 5-HT induced contraction of the guinea-pig ileum.
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The medium recommended by the European Pharmacopoeia (EP), 2nd edition, for the microbiological determination of neomycin by the agar diffusion method was tested and compared with the medium recommended by the EP, 1st edition. The tests were carried out in different laboratories. The medium recommended by the EP, 2nd edition, gave greater precision and reproducibility than the previous medium. The possibility of using a reference standard of almost pure neomycin B for both the determination of framycetin and neomycin was evaluated. The results demonstrated that the medium recommended by the EP, 2nd edition, gave better precision and reproducibility. Difficulty in achieving valid assays was practically the same with both media.
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Synthesis and antibacterial activity against Escherichia coli of a series of furazan sulfanilamides are reported. A structural activity relationship for these derivatives is also briefly discussed.
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