کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371398 | 981845 | 2011 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The rational design, syntheses and evaluation of potent sulfonamidopyrrolidin-2-one-based factor Xa inhibitors incorporating aminoindane and phenylpyrrolidine P4 motifs are described. These series delivered highly potent anticoagulant compounds with excellent oral pharmacokinetic profiles; however, significant time dependant P450 inhibition was an issue for the aminoindane series, but this was not observed with the phenylpyrrolidine motif, which produced candidate quality molecules with potential for once-daily oral dosing in humans.
The discovery of potent series of orally available factor Xa inhibitors with aminoindane and phenylpyrrolidine motifs is described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 6, 15 March 2011, Pages 1582–1587
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 6, 15 March 2011, Pages 1582–1587
نویسندگان
Robert J. Young, Carl Adams, Mike Blows, David Brown, Cynthia L. Burns-Kurtis, Chuen Chan, Laiq Chaudry, Máire A. Convery, David E. Davies, Anne M. Exall, Graham Foster, John D. Harling, Eric Hortense, Stephanie Irvine, Wendy R. Irving, Steve Jackson,