Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides.
Basic Information
ID: ALA2390941
Journal: Bioorg Med Chem Lett
Title: Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides.
Authors: Muench SP, Stec J, Zhou Y, Afanador GA, McPhillie MJ, Hickman MR, Lee PJ, Leed SE, Auschwitz JM, Prigge ST, Rice DW, McLeod R.
Abstract: 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.
CiteXplore: 23664871
DOI: 10.1016/j.bmcl.2013.04.035
Patent ID: ┄