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in vitro inhibition of the measles virus by novel ring-expanded ('fat') nucleoside analogues containing the imidazo[4,5-e]diazepine ring system.
Zhang, Ning; Chen, Huan-Ming; Sood, Ramesh; Kalicharran, Kishna; Fattom, Ali I; Naso, Robert B; Barnard, Dale L; Sidwell, Robert W; Hosmane, Ramachandra S.
Afiliación
  • Zhang N; Laboratory for Drug Design and Synthesis, Department of Chemistry and Biochemistry, University of Maryland, Baltimore County 21250, USA.
Bioorg Med Chem Lett ; 12(23): 3391-4, 2002 Dec 02.
Article en En | MEDLINE | ID: mdl-12419368
The synthesis and in vitro anti-measles virus (anti-MV) activity of a class of ring-expanded ('fat') nucleoside analogues (1-4) containing the title heterocyclic ring system are reported. The target compounds were synthesized by base-catalyzed condensations of 4,5-dicarboxylic acid esters of the appropriately substituted imidazole-1-ribosides with suitably substituted guanidine derivatives. Compounds were screened for anti-MV activity in African green monkey kidney cells (CV-1), employing ribavirin as the control standard. While the parent compound 1 itself failed to show any significant antiviral activity against MV, its analogues containing hydrophobic substituents at the 2-position (2) or the 6-position (4) showed promising antiviral activity at submicromolar or micromolar concentration levels with no apparent toxicity to the host cell line. Both compounds showed higher anti-MV activity than the control drug ribavirin.
Asunto(s)
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales / Virus del Sarampión / Nucleósidos Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2002 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales / Virus del Sarampión / Nucleósidos Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2002 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido