کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1379281 | 982022 | 2006 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex—Part 2
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
The activated factor VII/tissue factor complex (FVIIa/TF) is known to play a key role in the formation of blood clots. Inhibition of this complex may lead to new antithrombotic drugs. A fluoropyridine-based series of FVIIa/TF inhibitors was discovered which utilized a diisopropylamino group for binding in the S2 and S3 binding pockets of the active site of the enzyme complex. In this series, an enhancement in binding affinity was observed by substitution at the 5-position of the hydroxybenzoic acid sidechain. An X-ray crystal structure indicates that amides at this position may increase inhibitor binding affinity through interactions with the S1′/S2′ pocket.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 4, 15 February 2006, Pages 1060–1064
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 4, 15 February 2006, Pages 1060–1064
نویسندگان
Jeffrey T. Kohrt, Kevin J. Filipski, Wayne L. Cody, Cuiman Cai, Danette A. Dudley, Chad A. Van Huis, J. Adam Willardsen, Lakshmi S. Narasimhan, Erli Zhang, Stephen T. Rapundalo, Kamlai Saiya-Cork, Robert J. Leadley, Jeremy J. Edmunds,