کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10591715 | 981760 | 2013 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Development of a triclosan scaffold which allows for adaptations on both the A- and B-ring for transport peptides
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 12, 15 June 2013, Pages 3551-3555
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 12, 15 June 2013, Pages 3551-3555
نویسندگان
Stephen P. Muench, Jozef Stec, Ying Zhou, Gustavo A. Afanador, Martin J. McPhillie, Mark R. Hickman, Patty J. Lee, Susan E. Leed, Jennifer M. Auschwitz, Sean T. Prigge, David W. Rice, Rima McLeod,