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An orally bioavailable oxime ether capsid binder with potent activity against human rhinovirus.
Watson, Keith G; Brown, Renee N; Cameron, Rachel; Chalmers, David K; Hamilton, Stephanie; Jin, Betty; Krippner, Guy Y; Luttick, Angela; McConnell, Darryl B; Reece, Phillip A; Ryan, Jane; Stanislawski, Pauline C; Tucker, Simon P; Wu, Wen-Yang; Barnard, Dale L; Sidwell, Robert W.
Afiliação
  • Watson KG; Biota Chemistry Laboratory, School of Chemistry, Monash University, PO Box 23 Victoria, Australia 3800. kwatson@wehi.edu.au
J Med Chem ; 46(15): 3181-4, 2003 Jul 17.
Article em En | MEDLINE | ID: mdl-12852746
ABSTRACT
A series of capsid-binding compounds was screened against human rhinovirus (HRV) using a CPE based assay. The ethyl oxime ether 14 was found to have outstanding anti-HRV activity (median IC(50) 4.75 ng/mL), and unlike the equivalent ethyl ester compound 3 (Pirodavir), it has good oral bioavailability, making it a promising development candidate. Compound 14 illustrates that an oxime ether group can act as a metabolically stable bioisostere for an ester functionality.
Assuntos
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Antivirais / Oximas / Rhinovirus / Capsídeo Limite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2003 Tipo de documento: Article
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Antivirais / Oximas / Rhinovirus / Capsídeo Limite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2003 Tipo de documento: Article