کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358510 | 981346 | 2013 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of derivatives of the keto-pyrrolyl-difluorophenol scaffold: Some structural aspects for aldose reductase inhibitory activity and selectivity
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Seven novel ARIs (3a–c, 4a–c and 5) were synthesized with the implementation of an optimized and, partially, selective synthetic procedure, via a Friedel–Crafts acylation reaction. The synthesized ARIs have values of IC50ALR2 ranging from 0.19 μM (in case of compound 3b) to 2.3 μM (in case of compound 4a), while the values of selectivity index towards ALR1 range from 1 (in case of compound 3b) to 238 (in case of compound 3a). Finally, we found out that the presence of an additional (secondary) aromatic area is not a prerequisite feature for ARI activity.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 4, 15 February 2013, Pages 869–873
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 4, 15 February 2013, Pages 869–873
نویسندگان
Eleni Kotsampasakou, Vassilis J. Demopoulos,