کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1379372 | 982027 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold](/preview/png/1379372.png)
چکیده انگلیسی
Imidazole-based structures of p38 inhibitors served as a starting point for the design of JNK3 inhibitors. Construction of a 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold led to the synthesis of the (S)-enantiomers, which exhibited p38/JNK3 IC50 ratio of up to 10 and were up to 20 times more potent inhibitors of JNK3 than the relevant (R)-enantiomers. The JNK3 inhibitory potency correlated well with inhibition of c-Jun phosphorylation and neuroprotective properties of the compounds in low K+-induced cell death of rat cerebellar granule neurones.
The synthesis and neuroprotective properties of three representative enantiomeric pairs (S)-2 and (R)-2 are reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 21, 1 November 2005, Pages 4666–4670
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 21, 1 November 2005, Pages 4666–4670
نویسندگان
Piotr P. Graczyk, Afzal Khan, Gurpreet S. Bhatia, Vanessa Palmer, Darren Medland, Hirotoshi Numata, Hitoshi Oinuma, Jacqueline Catchick, Angela Dunne, Moira Ellis, Caroline Smales, Jonathan Whitfield, Stephen J. Neame, Bina Shah, Daniel Wilton,