کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587710 | 981436 | 2013 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and biological activity of diaryl ether inhibitors of Toxoplasma gondii enoyl reductase
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Design, synthesis, and biological activity of diaryl ether inhibitors of Toxoplasma gondii enoyl reductase Design, synthesis, and biological activity of diaryl ether inhibitors of Toxoplasma gondii enoyl reductase](/preview/png/10587710.png)
چکیده انگلیسی
Triclosan is a potent inhibitor of Toxoplasma gondii enoyl reductase (TgENR), which is an essential enzyme for parasite survival. In view of triclosan's poor druggability, which limits its therapeutic use, a new set of B-ring modified analogs were designed to optimize its physico-chemical properties. These derivatives were synthesized and evaluated by in vitro assay and TgENR enzyme assay. Some analogs display improved solubility, permeability and a comparable MIC50 value to that of triclosan. Modeling of these inhibitors revealed the same overall binding mode with the enzyme as triclosan, but the B-ring modifications have additional interactions with the strongly conserved Asn130.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 7, 1 April 2013, Pages 2035-2043
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 7, 1 April 2013, Pages 2035-2043
نویسندگان
Gang Cheng, Stephen P. Muench, Ying Zhou, Gustavo A. Afanador, Ernest J. Mui, Alina Fomovska, Bo Shiun Lai, Sean T. Prigge, Stuart Woods, Craig W. Roberts, Mark R. Hickman, Patty J. Lee, Susan E. Leed, Jennifer M. Auschwitz, David W. Rice, Rima McLeod,