RESUMEN
The 5'-triphosphate of 5-nitroindole-2'-deoxyriboside has been shown to be a good substrate for terminal deoxynucleotidyl transferase (TdT). An antibody has been prepared for the detection of 5-nitroindole and has been used for the detection of 5-nitroindole tailed DNA both in single-stranded form and after hybridisation to a template. This is therefore a new method for the detection of nucleic acid probes.
Asunto(s)
Indoles , Indoles/química , Oligonucleótidos/análisis , Anticuerpos/metabolismo , ADN Nucleotidilexotransferasa/metabolismo , Sondas de ADN/química , Nucleótidos de Desoxiadenina , Indoles/inmunología , Indoles/metabolismo , Espectroscopía de Resonancia Magnética , Estructura Molecular , Hibridación de Ácido NucleicoRESUMEN
The synthesis and antibacterial activity of 6 alpha-methoxysulbenicillin analogues (2) are described. Structure-activity studies of these derivatives bearing hydrophilic substituents in the phenyl ring led to the identification of disodium 6 beta-[D-2-(3,4-dihydroxyphenyl)-2-sulfoacetamido]-6 alpha-methoxypenicillanate (2m) as a compound with potent activity against Pseudomonas aeruginosa including beta-lactamase producing strains. Additional substitution of 2m gave derivatives 2p, 2q, 2r, with a further improvement in activity against Gram-negative bacteria.
Asunto(s)
Penicilina G/análogos & derivados , Sulbenicilina/análogos & derivados , Fenómenos Químicos , Química , Enterobacteriaceae/efectos de los fármacos , Pruebas de Sensibilidad Microbiana , Resistencia a las Penicilinas , Pseudomonas aeruginosa/efectos de los fármacos , Relación Estructura-Actividad , Sulbenicilina/síntesis química , Sulbenicilina/farmacologíaRESUMEN
The influence on the antibacterial activity of introducing a 6 alpha-methoxy group into carbenicillin, and various 6 alpha-substituents into sulbenicillin and piperacillin was examined. Further variations of the side chain aryl group were examined in the 6 alpha-methoxy substituted series. This led to the identification of disodium 6 beta-(D,L-2-carboxy-2-thien-3-ylacetamido)-6 alpha-methoxypenicillanate (5b) as a beta-lactamase stable derivative with useful activity against Enterobacteriaceae, and disodium 6 beta-[D-2-(4-aminophenyl)-2-sulfoacetamido]-6 alpha-methoxypenicillanate (6e) with slightly lower activity against the Enterobacteriaceae but more active against Pseudomonas aeruginosa.