The pharmacological properties of the tetrazole analogues of ibuprofen and flurbiprofen are reported.
Teîrezol-Analoge des Ibuprofens und FiurbiprofensTetrazol-Analoga des Ibuprofens und Flurbiprofens und ihre pharmakologischen Eigenschaften werden beschrieben.Tetrazole derivatives, apart the wel1 known leptazol, have received in the past decade an increasing interest amongst medicinal chemists as may be seen in a recent review that covers this literature until 1980'). Since the acid strenght of this heterocycle with free NH is comparable to that of aliphatic carboxylic acid, its bioisosteric replacement in a number of drugs bearing a carboxy group has been successfully experienced'). This modification is often attempted in order to eliminate unwanted side effects or to potcntiate some components of the pharmacological spectrum of the parent drug.We refer in this note the potentiation of the analgesic effect induced by the tetrazole analogues of ibuprofen (1) and flurbiprofen (2).These compounds were prepared as usual by reacting the corresponding nitrile derivatives with sodium azide2).
Pharmacology Methods
Acute toxicity:Male albino mice, 25-30 g, were given the test compounds suspended in 10 % acacia by moiith. Approximate LD50 values were determined by inspection from mortalities occurring within 7 days. Animals always showed acute signs of prostration and sedation and death occurred mainly from perforated gastric ulcers, in agreement with the typical ulcerogenic properties of the non steroidal anti-inflammatory agents.
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Cholinergic Agents. Synthesis and Acetylcholinesterase Inhibitory Activity of Some ω-(N-Methyl-N-(3-alkylcarbamoyloxyphenyl)methyl)aminoalkoxyxanthen-9-ones.-A series of the title xanthone derivatives such as (IX) (10 examples) is synthesized and evaluated for their acetylcholinesterase inhibitory activity. -(VALENTI, P.; RAMPA, A.; BISI, A.; FABBRI, G.; ANDRISANO, V.; CAVRINI, V.; Med. Chem. Res. 5 (1995) 4, 255-264; Dep. Pharm. Sci., Univ., I-40126 Bologna, Italy; EN)
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