کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369956 | 981799 | 2012 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of 4-alkynyl pyrazoles as inhibitors of PDE4: A practical access via Pd/C–Cu catalysis
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The design and synthesis of 4-alkynyl pyrazole derivatives has led to the identification of new class of PDE4 inhibitors. All these compounds were accessed for the first time via a facile Pd/C–CuI–PPh3 mediated C–C bond forming reaction between an appropriate pyrazole iodide and various terminal alkynes. In vitro PDE4B inhibitory properties and molecular modeling studies of some of the compounds synthesized indicated that 4-alkynyl pyrazole could be a promising template for the discovery of novel PDE4 inhibitors.
Design, synthesis, PDE4 inhibitory properties along with docking studies of new 4-alkynyl pyrazoles is presented.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 7, 1 April 2012, Pages 2480–2487
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 7, 1 April 2012, Pages 2480–2487
نویسندگان
Dhilli Rao Gorja, K. Shiva Kumar, Ajit Kandale, Chandana Lakshmi T. Meda, Kishore V.L. Parsa, K. Mukkanti, Manojit Pal,