1438425-41-2Relevant academic research and scientific papers
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
, p. 3551 - 3555 (2013/07/04)
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.
