RESUMO
Chondrosarcoma is a tumor very seldom encountered in the larynx. In this location chondrosarcomas have typical features: slow growing, metastasis rares and scarce tendency to recur. But recurrences occurs at long-term and often can be controlled. We report a case diagnosed and treated in our Hospital which, on the contrary, recurrences presented in a short-term after first surgical removal. Clinical management and treatment of these neoplasms are reviewed.
Assuntos
Condrossarcoma/diagnóstico por imagem , Condrossarcoma/patologia , Neoplasias Laríngeas/diagnóstico por imagem , Neoplasias Laríngeas/patologia , Adulto , Condrossarcoma/cirurgia , Humanos , Neoplasias Laríngeas/cirurgia , Masculino , Estadiamento de Neoplasias , Tomografia Computadorizada por Raios XRESUMO
Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field.
Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Cetonas/síntese química , Cetonas/farmacologia , Metanol/análogos & derivados , Nitroimidazóis/síntese química , Nitroimidazóis/farmacologia , Testes de Sensibilidade Microbiana , Testes de Mutagenicidade , Relação Estrutura-AtividadeRESUMO
Four series of compounds whose substructure contains a formamidine functionalized as a novel group in the chemistry of histamine H2-receptors have been synthesized. Series design, synthesis and pharmacological data including inhibition of histamine-stimulated acid secretion, inhibition of acid secretion p.o. and pA2 are reported. N-[(E)-[[2-[[[2](Diaminomethylene)amino]-4-thiazolyl] methyl]thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamide (ebrotidine, CAS 100981-43-9, FI-3542) was selected for further research.
Assuntos
Amidinas/síntese química , Antagonistas dos Receptores H2 da Histamina/síntese química , Amidinas/farmacologia , Animais , Depressão Química , Feminino , Ácido Gástrico/metabolismo , Cobaias , Átrios do Coração/efeitos dos fármacos , Frequência Cardíaca/efeitos dos fármacos , Antagonistas dos Receptores H2 da Histamina/farmacologia , Técnicas In Vitro , Masculino , Ratos , Ratos Sprague-Dawley , Relação Estrutura-AtividadeRESUMO
Ebrotidine (N-[(E)-[[2-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl] thio]ethyl]amino]methylene]-4-bromo-benzenesulfonamide, CAS 100981-43-9, FI-3542) is a new H2-receptor antagonist with a potent antisecretory activity and evidenced gastroprotection. This paper describes its physicochemical properties, spectroscopy for its structural identification, detection methods for its organic and inorganic impurities, purity quantitation and stressed degradation and stability tests in solid and solution forms in order to know the behaviour of the test substance against certain experimental conditions. The results obtained indicate that ebrotidine is stable for over 3 years normal storage conditions (25 degrees C/75% RH). As ebrotidine was not found to be hygroscopic or particularly photosensitive, no special storage precautions are required.
Assuntos
Benzenossulfonatos/química , Antagonistas dos Receptores H2 da Histamina/química , Tiazóis/química , Cromatografia Líquida de Alta Pressão , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Potenciometria , Espectrofotometria Ultravioleta , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios XRESUMO
Compound 1 (1-benzyl-3-methyl-4-[4-(4-fluorophenyl)-4-oxobutyl]piperazine), a synthetic intermediate identified as a potential atypical antipsychotic, was selected as the starting point for pharmacological improvement. From 1, sequential structural variations were conducted in order to improve its potency and oral bioavailability. These variations included a series of piperazine, ethanediamine, and piperidine derivatives. The piperidine series afforded some orally potent compounds in the inhibition of apomorphine-induced climbing and hyperactivity in mice, which are regarded as behavioral models predictive of antipsychotic efficacy. Further optimization of these structures led to the highly potent 7-[3-(1-piperidinyl)propoxy]chromenones. Inhibition of stereotypies and induction of catalepsy in rats at doses substantially higher than required for inhibition of climbing suggest an atypical antipsychotic profile, which is assumed to predict a reduced induction of extrapyramidal side effects in humans.
Assuntos
Antipsicóticos/síntese química , Cromonas/síntese química , Administração Oral , Animais , Antipsicóticos/farmacocinética , Antipsicóticos/farmacologia , Apomorfina/farmacologia , Comportamento Animal/efeitos dos fármacos , Disponibilidade Biológica , Catalepsia/induzido quimicamente , Cromonas/farmacocinética , Cromonas/farmacologia , Masculino , Camundongos , Estrutura Molecular , Atividade Motora/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Comportamento Estereotipado/efeitos dos fármacos , Relação Estrutura-AtividadeRESUMO
A new series of (benzo[b]thienyl)methyl ethers of 1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethanol and of (Z)-1-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl)ethanone oxime were synthesis and tested for antifungal activity. Series design, synthesis, preliminary antimycotic data and structure-activity relationships are reported. 7-Chloro-3-[1-(2,4-dichlorophenyl)-2-(1H-imidazol-1- yl)ethoxymethyl]benzo[b] (8i, Sertaconazole, FI-7045, CAS 99592-32-2) and its nitrate were selected for further research.
