RESUMO
Cultures of actinomycete strain WRAT-210 produced a dark red crystalline metabolite which was named texazone. Spectroscopic evidence suggested that the structure of texazone is 2-(N-methylamino)-3H-phenoxazin-3-one-8-carboxylic acid. The structure was confirmed by chemical synthesis through oxidative dimerization of ethyl 3-amino-4-hydroxybenzoate with 2-(N-methylamino)phenol and subsequent hydrolysis of the resultant phenoxazinone ester.
Assuntos
Actinomyces/metabolismo , Antibacterianos/biossíntese , Oxazinas/biossíntese , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Oxazinas/isolamento & purificação , EspectrofotometriaRESUMO
Amongst a series of novel derivatives of N,N-bis-(alpha, alpha, alpha-trifluoro-m-tolyl)amine, several were found to possess antiinflammatory, hypotensive, antibacterial and antifungal activity. The synthesis of these compounds is described and their biological properties are discussed.
Assuntos
Compostos de Anilina/síntese química , Difenilamina/síntese química , Animais , Anti-Infecciosos/síntese química , Anti-Inflamatórios/síntese química , Antifúngicos/síntese química , Anti-Hipertensivos/síntese química , Difenilamina/análogos & derivados , Difenilamina/farmacologia , Cobaias , Técnicas In Vitro , RatosRESUMO
A number of new esters of fluphenazine are described: among these was the 1-adamantoate, 1h, the first highly crystalline ester of that drug. The 1-adamantoate of pipotiazine, 2b, typically, was an oil. Following a single subcutaneous or intramuscular injection of 25 mg/kg of either 1h or 2b, dissolved in sesame oil, each ester was found to be a potent and long-acting inhibitor of conditioned avoidance behavior in the rat.
