کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10595168 | 981861 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability](/preview/png/10595168.png)
چکیده انگلیسی
A series of potent carboxylic acid DGAT1 inhibitors with high permeability were developed from a virtual screening hit. Strategies were employed to reduce Pgp substrate recognition and increase passive permeability, resulting in the discovery of a series showing good inhibition of cellular triglyceride synthesis. The mutagenic potential of prospective metabolites was evaluated in the Ames assay, and one aniline was shown to be devoid of mutagenicity.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 2, 15 January 2012, Pages 824-828
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 2, 15 January 2012, Pages 824-828
نویسندگان
Ustav Bali, Oscar Barba, Graham Dawson, William T. Gattrell, James G. Horswill, David A. Pan, Martin J. Procter, Chrystelle M. Rasamison, Colin P. Sambrook Smith, Amanda Taylor-Warne, Philippe Wong-Kai-In,