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Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides.
Muench, Stephen P; Stec, Jozef; Zhou, Ying; Afanador, Gustavo A; McPhillie, Martin J; Hickman, Mark R; Lee, Patty J; Leed, Susan E; Auschwitz, Jennifer M; Prigge, Sean T; Rice, David W; McLeod, Rima.
Afiliação
  • Muench SP; School of Biomedical Sciences, University of Leeds, Leeds, UK. s.p.muench@leeds.ac.uk
Bioorg Med Chem Lett ; 23(12): 3551-5, 2013 Jun 15.
Article em En | MEDLINE | ID: mdl-23664871
The enoyl acyl-carrier protein reductase (ENR) enzyme is harbored within the apicoplast of apicomplexan parasites providing a significant challenge for drug delivery, which may be overcome through the addition of transductive peptides, which facilitates crossing the apicoplast membranes. The binding site of triclosan, a potent ENR inhibitor, is occluded from the solvent making the attachment of these linkers challenging. Herein, we have produced 3 new triclosan analogs with bulky A- and B-ring motifs, which protrude into the solvent allowing for the future attachment of molecular transporters for delivery.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Triclosan / Proteínas de Transporte / Enoil-(Proteína de Transporte de Acila) Redutase (NADH) Idioma: En Ano de publicação: 2013 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Triclosan / Proteínas de Transporte / Enoil-(Proteína de Transporte de Acila) Redutase (NADH) Idioma: En Ano de publicação: 2013 Tipo de documento: Article