کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372123 | 981865 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel small molecule bradykinin B1 receptor antagonists. Part 1: Benzamides and semicarbazides
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Novel small molecule bradykinin B1 receptor antagonists. Part 1: Benzamides and semicarbazides Novel small molecule bradykinin B1 receptor antagonists. Part 1: Benzamides and semicarbazides](/preview/png/1372123.png)
چکیده انگلیسی
The synthesis and SAR of two series of bradykinin B1 receptor antagonists is described. The benzamide moiety proved to be a suitable replacement for the aryl ester functionality of biaryl based antagonists. In addition, it was found that semicarbazides can effectively replace cyclopropyl amino acids. The compounds with the best overall profile were biaryl semicarbazides which display high antagonistic activity, low Caco-2 efflux and high oral bioavailability in the rat.
Benzamides and semicarbazides are introduced as new classes of bradykinin B1 receptor antagonists. The best compounds feature excellent pharmacokinetic properties in the rat.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 3, 1 February 2010, Pages 1225–1228
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 3, 1 February 2010, Pages 1225–1228
نویسندگان
Marco Schaudt, Elsa Locardi, Gunther Zischinsky, Roland Stragies, Jochen R. Pfeifer, Christoph Gibson, Dirk Scharn, Uwe Richter, Holger Kalkhof, Klaus Dinkel, Karsten Schnatbaum,