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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
The development of first Staphylococcus aureus SplB protease inhibitors: Phosphonic analogues of glutamine
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 M−1 s−1.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 17, 1 September 2012, Pages 5574-5578
نویسندگان
, , , , , , ,