کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10594621 | 981836 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The development of first Staphylococcus aureus SplB protease inhibitors: Phosphonic analogues of glutamine
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Produced by Staphylococcus aureus, SplB belongs to the chymotrypsin-like serine protease family. Since the biological role of SplB protease is unknown, the design and application of its specific inhibitors may help to reveal the function of this enzyme. Until now no SplB inhibitors have been reported. Herein, we present the design and synthesis of novel α-aminophosphonic analogues of glutamine, as well as their peptidyl derivatives. The inhibitory effects of these compounds towards the newly discovered SplB serine protease from S. aureus are characterized. We have also investigated the influence of aromatic ester substituents on inhibitory potency towards SplB. One of the compounds-Cbz-Glu-Leu-GlnP(OC6H4-4-O-CH3)2-displayed an apparent second-order inhibition rate value of 1400 Mâ1 sâ1.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 17, 1 September 2012, Pages 5574-5578
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 17, 1 September 2012, Pages 5574-5578
نویسندگان
Burchacka Ewa, Walczak Maciej, SieÅczyk Marcin, Dubin Grzegorz, Zdżalik MichaÅ, Potempa Jan, Oleksyszyn Józef,