Bioorganic & Medicinal Chemistry Letters 1991-06-01

Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides.

F T Delbeke, M Debackere, L Vynckier

文献索引：Bioorg. Med. Chem. Lett. 23(12) , 3551-5, (2013)

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摘要

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.Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.