کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377649 | 981984 | 2006 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Aggrecanases are recently discovered enzymes that cleave aggrecan, a key component of cartilage. Aggrecanase inhibitors may provide a unique means to halt the progression of cartilage destruction in osteoarthritis. The synthesis and evaluation of biphenylsulfonamidocarboxylic acid inhibitors of aggrecanase-1 are reported. Compound 24 demonstrated 89% inhibition of proteoglycan degradation at 10 μg/mL and has an oral bioavailability in rat of 35%.
The synthesis and evaluation of biphenylsulfonamidocarboxylic acid inhibitors of aggrecanase-1 are reported. Compound 24 demonstrated 89% inhibition of proteoglycan degradation at 10 μg/mL and has an oral bioavailability in rat of 35%.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 2, 15 January 2006, Pages 311–316
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 2, 15 January 2006, Pages 311–316
نویسندگان
Jason S. Xiang, Yonghan Hu, Thomas S. Rush, Jennifer R. Thomason, Manus Ipek, Phaik-Eng Sum, Leila Abrous, Joshua J. Sabatini, Katy Georgiadis, Erica Reifenberg, Manas Majumdar, Elisabeth A. Morris, Steve Tam,