RESUMO
Two polar metabolites of mitoxantrone, a clinically active antitumor agent, have been isolated and purified from the urine of patients by sequential absorption on glass wool and C18-Sep-Pak cartridges followed by preparative high-performance liquid chromatography. Negative ion chemical ionization mass spectrometry indicated that the two metabolites are the di- and mono-carboxylic acids resulting from oxidation of the terminal hydroxyl groups of the side chain(s). Mass spectral comparison of the urinary metabolites with synthetic compounds confirmed the identification.
Assuntos
Antraquinonas/urina , Antraquinonas/metabolismo , Cromatografia Líquida de Alta Pressão , Humanos , Espectrometria de Massas , MitoxantronaRESUMO
Several formamidine and acetamidine derivatives prepared from 3-amino-1,2,4-benzotriazine and 3-amino-1,2,4-benzotriazine-1-oxide displayed an aspirin-like anti-inflammatory and analgesic profile. The test systems include adjuvant-induced arthritis in rats, carrageenan-induced edema in rats, UV-induced erythema in guinea pigs, the analgesic gait test, the antipyretic test, and GI ulcer studies.
Assuntos
Anti-Inflamatórios não Esteroides/síntese química , Triazinas/farmacologia , Animais , Anti-Inflamatórios não Esteroides/uso terapêutico , Artrite Experimental/tratamento farmacológico , Carragenina , Fenômenos Químicos , Química , Relação Dose-Resposta a Droga , Edema/induzido quimicamente , Edema/tratamento farmacológico , Eritema/tratamento farmacológico , Cobaias , Ratos , Úlcera Gástrica/induzido quimicamente , Triazinas/síntese química , Triazinas/uso terapêuticoRESUMO
Benzoylacetonitrile and beta-aminocinnamonitrile are shown to possess potent antiinflammatory activity in the rat adjuvant arthritis model. In a series of phenyl-substituted analogues, only o-, m-, and p-fluorobenzoylacetonitrile and m- and p-fluoro-beta-aminocinnamonitrile retained activity. Additionally, beta-amino-2- and beta-amino-3-thiopheneacrylonitrile and beta-oxo-2- and beta-oxo-3-thiophenepropionitrile exhibited similar activity. These agents are not believed to be acting via prostaglandin synthetase inhibition. The metabolic profile of benzoylacetonitrile is also described.
