کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10592325 | 981788 | 2014 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Bioisosteres are integral components of modern pharmaceutical research that allow structural optimization to maximize in vivo efficacy and minimize adverse effects by selectively modifying pharmacodynamic, pharmacokinetic and physicochemical properties. A recent medicinal chemistry campaign focused on identifying small molecule inhibitors of prolylcarboxypeptidase (PrCP) initiated an investigation into the use of pyrazoles as bioisosteres for amides. The results indicate that pyrazoles are suitable bioisosteric replacements of amide functional groups. The study is an example of managing bioisosteric replacement by incorporating subsequent structural modifications to maintain potency against the selected target. A heuristic model for an embedded pharmacophore is also described.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 7, 1 April 2014, Pages 1657-1660
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 7, 1 April 2014, Pages 1657-1660
نویسندگان
Thomas H. Graham, Min Shu, Andreas Verras, Qing Chen, Margarita Garcia-Calvo, Xiaohua Li, JeanMarie Lisnock, Xinchun Tong, Elaine C. Tung, Judyann Wiltsie, Jeffrey J. Hale, Shirly Pinto, Dong-Ming Shen,