RESUMEN
The E and Z isomers of 2-[2-(3-chlorophenyl)-1-phenyl-1-propenyl]pyridine (2a,b) and 2-[2-(3-chlorophenyl)-1-(4-hydroxyphenyl)-1-propenyl]pyridine (4a,b) were synthesized and separated as possible metabolites of 1-(3-chlorophenyl)-1-methyl-2-phenyl-2-(2-pyridine)ethanol (1a). Following administration of 1a to rats, a HPLC system was used to examine urine and serum specimens for the less polar metabolites of 1a. Isomers 2a and 2b were not detected but their hydroxylated derivatives 4a and 4b were observed as minor metabolites. Compounds 2a,b and 4a,b exhibited hypocholesteremic activity in rats; compounds 4a and 4b are of special interest because they possessed relatively low estrogenicity.
Asunto(s)
Anticolesterolemiantes/síntesis química , Piridinas/síntesis química , Animales , Anticolesterolemiantes/metabolismo , Castración , Cromatografía Líquida de Alta Presión , Congéneres del Estradiol/síntesis química , Femenino , Masculino , Piridinas/metabolismo , Piridinas/farmacología , Ratas , EstereoisomerismoRESUMEN
5 beta-Tetrahydro-Reichstein's Substance S (3 alpha, 5 beta-THS) from different sources yielded variable bioassay activity in the chick chorio-allantoic membrane assay system. Physical characterization showed impure products. Synthesis of this compound by two different routes yielded active and inactive 3 alpha, 5 beta-THS. Of the other two epimers, 3 beta, 5 beta-THS (epi-THS) and 3 alpha, 5 alpha-THS (allo-THS), only the latter was active. These results suggest that the impurities present in 3 alpha, 5 beta-THS synthesized by reduction of the alpha, beta-unsaturated ketone of Substance S might be either or both the epi-/allo-epimers (3 beta, 5 beta-THS and 3 alpha, 5 alpha-THS, respectively), with only the latter contributing the positive angiostatic activity to the mixture. Of the two synthetically derived compounds, only the latter was shown to maintain the activity, whereas 3 alpha, 5 beta-THS was not antiangiogenic.
Asunto(s)
Cortodoxona/análogos & derivados , Alantoides/irrigación sanguínea , Alantoides/efectos de los fármacos , Animales , Embrión de Pollo , Corion/irrigación sanguínea , Corion/efectos de los fármacos , Cromatografía Líquida de Alta Presión , Cortodoxona/síntesis química , Cortodoxona/química , Cortodoxona/farmacología , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Estructura Molecular , Oxidación-Reducción , Espectroscopía Infrarroja por Transformada de Fourier , EstereoisomerismoRESUMEN
This paper presents pragmatic particulars pertaining to plume protection problems with special emphasis on the health care environment. Practical approaches to optimizing protection are discussed with an eye toward facilitating the safety of personnel and the general health care environment from particulates, parasites, viruses and other undesirable entities, elements and compounds.