Assuntos
Heparina/farmacocinética , Absorção Intestinal , Animais , Inibidores do Fator Xa , Masculino , RatosRESUMO
A number of 3-carbonylacrylic acid derivatives were prepared, with a view to varying systematically the stereoelectronic environment of the conjugated double bond. The rates of reaction with cysteine were measured spectrophotometrically when possible or by stopped flow when very fast. Some of the final reaction products were isolated. Other properties examined were partition substituent constants and antimicrobial activity. On the basis of published data and these studies, the activity appears to be the combined effect of at least two mechanisms, one probably related to the effect of these structures on surface tension, the other to the electrophilic properties of the unsaturated system.
Assuntos
Acrilatos/farmacologia , Anti-Infecciosos/síntese química , Cisteína/metabolismo , Antibacterianos , Anti-Infecciosos/farmacologia , Espectroscopia de Ressonância Magnética , Microsporum/efeitos dos fármacos , Espectrofotometria , Staphylococcus aureus/efeitos dos fármacos , Relação Estrutura-AtividadeRESUMO
Eight new aroyl-acrylic esters of polyethylene glycols were prepared using different synthetic ways. They are supposed to possess a higher activity as antimicotic agents for topical use, by favouring skin absorption. Except in few cases, the antimicrobial activity of the oligomeric derivatives resulted generally decreased in vitro, in comparison to simple alkyl esters previously prepared. However, only pharmacological screenings for antimicotic activity in vivo will give a definite response on whether the new derivatives are advantageous for topical use.
Assuntos
Acrilatos/síntese química , Anti-Infecciosos/síntese química , Antifúngicos/síntese química , Polietilenoglicóis/síntese química , Acrilatos/farmacologia , Fenômenos Químicos , Química , Cromatografia em Camada Fina , Testes de Sensibilidade Microbiana , Polietilenoglicóis/farmacologiaRESUMO
The ability of a new anticonvulsant drug, denzimol, to interact with bovine serum proteins has been studied, in comparison with diphenylhydantoin and carbamazepine. Albumin proved to be the protein fraction responsible for the binding. The association constants were determined in vitro by means of equilibrium dialysis. Additional investigations showed that there was no consistent inhibition by denzimol of the other two drugs binding and vice versa. These data were obtained as a preliminary evaluation of the influence of protein binding in vivo.
