RESUMEN
New N¹-benzyl esters of N¹-oxide analogues of 5'-noraristeromycin were synthesized and tested as potential inhibitors of S-adenosyl-L-homocysteine hydrolase in Vaccinia virus infected cell systems.
Asunto(s)
Adenosina/análogos & derivados , Antivirales/síntesis química , Antivirales/farmacología , Virus Vaccinia , Vaccinia/tratamiento farmacológico , Adenosina/síntesis química , Adenosina/química , Adenosina/farmacología , Animales , Antivirales/química , Chlorocebus aethiops , Evaluación Preclínica de Medicamentos , Humanos , Células VeroRESUMEN
N-(9-Fluorenylmethoxycarbonyl)-omega-aminoalkyl, N-(9-fluorenylmethoxycarbonyl)-8-amino-3,6-dioxaoctyl, and N-(9-fluorenylmethoxycarbonyl)-6-aminohexanoyl]-2-aminoethyl triphosphates were synthesized. All of them were shown to be the substrates of the calf thymus terminal deoxynucleotidyl transferase. Their substrate properties depend on the length and structure of linker between the 9-fluorenylmethoxycarbonyl and triphosphate moieties.
Asunto(s)
ADN Nucleotidilexotransferasa/metabolismo , Organofosfatos/síntesis química , Animales , Bovinos , Cromatografía por Intercambio Iónico , Estructura Molecular , Organofosfatos/química , Organofosfatos/farmacología , Relación Estructura-Actividad , Especificidad por Sustrato , Timo/enzimologíaRESUMEN
New 5'-alkyl ethoxy- and aminocarbonylphosphonates of 3'-azido-3'-deoxythymidine (AZT) were synthesized, and their antiviral properties in HIV-1-infected cell cultures and stability to chemical hydrolysis were studied. The AZT 5'-aminocarbonylphosphonates were shown to be significantly more stable in phosphate buffer (pH 7.2) than the corresponding ethoxycarbonylphosphonates. The therapeutic (selectivity) index of some of the compounds exceeded that of the parent AZT due to their higher antiviral activity. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2004, vol. 30, no. 3; see also http://www.maik.ru.
