کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373364 | 1500544 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The discovery and structure–activity relationships of indole-based inhibitors of glutamate carboxypeptidase II
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: The discovery and structure–activity relationships of indole-based inhibitors of glutamate carboxypeptidase II The discovery and structure–activity relationships of indole-based inhibitors of glutamate carboxypeptidase II](/preview/png/1373364.png)
چکیده انگلیسی
A series of N-substituted 3-(2-mercaptoethyl)-1H-indole-2-carboxylic acids were synthesized as inhibitors of glutamate carboxypeptidase II (GCPII). Those containing carboxybenzyl or carboxyphenyl groups at the N-position exhibited potent inhibitory activity against GCPII. These indole-based compounds represent the first example of achiral GCPII inhibitors and demonstrate greater tolerance of the GCPII active site for ligands with significant structural difference from the endogenous substrate, N-acetyl-aspartylglutamate.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 24, 15 December 2010, Pages 7222–7225
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 24, 15 December 2010, Pages 7222–7225
نویسندگان
Brian Grella, Jessica Adams, James F. Berry, Greg Delahanty, Dana V. Ferraris, Pavel Majer, Chiyou Ni, Krupa Shukla, Scott A. Shuler, Barbara S. Slusher, Marigo Stathis, Takashi Tsukamoto,