کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373143 | 981891 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of β-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of β-aminoacyl containing thiazolidine derivatives was synthesized and evaluated for their ability to inhibit DPP-IV. Several thiazolidine derivatives with an acid moiety were found to be potent DPP-IV inhibitors. Among them, compound 2da is the most active in this series with an IC50 value of 1 nM, and it showed excellent selectivity over DPP-IV related enzymes including DPP-2, DPP-8, and DPP-9. Compound 2da is chemically and metabolically stable, and showed no CYP inhibition, hERG binding or cytotoxicity. Compound 2db, an ester prodrug of 2da, showed good in vivo DPP-IV inhibition after oral administration in rat and dog models.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1366–1370
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1366–1370
نویسندگان
Woul Seong Park, Seung Kyu Kang, Mi Ae Jun, Mi Sik Shin, Ki Young Kim, Sang Dal Rhee, Myung Ae Bae, Min Sun Kim, Kwang Rok Kim, Nam Sook Kang, Sung-eun Yoo, Jie Oh Lee, Dong Hyun Song, Peter Silinski, Stephen Edward Schneider, Jin Hee Ahn, Sung Soo Kim,