کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2474734 1113160 2014 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Novel coumarin–benzimidazole derivatives as antioxidants and safer anti-inflammatory agents
ترجمه فارسی عنوان
مشتقات کومارینا بنزیمیدازول به عنوان آنتی اکسیدان ها و عوامل ضد التهابی مطمئن تر
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
چکیده انگلیسی

Inspired from occurrence of anti-inflammatory activity of 3-substituted coumarins and antiulcer activity of various 2-substituted benzimidazoles, novel compounds have been designed by coupling coumarin derivatives at 3-position directly or through amide linkage with benzimidazole nucleus at 2-position. The resultant compounds are expected to exhibit both anti-inflammatory and antioxidant activities along with less gastric toxicity profile. Two series of coumarin–benzimidazole derivatives (4a–e and 5a–e) were synthesized and evaluated for anti-inflammatory activity and antioxidant activity. Compounds 4c, 4d and 5a displayed good anti-inflammatory (45.45%, 46.75% and 42.85% inhibition, respectively, versus 54.54% inhibition by indomethacin) and antioxidant (IC50 of 19.7, 13.9 and 1.2 µmol/L, respectively, versus 23.4 µmol/L for butylatedhydroxytoluene) activities. Evaluation of ulcer index and in vivo biochemical estimations for oxidative stress revealed that compounds 4d and 5a remain safe on gastric mucosa and did not induce oxidative stress in tissues. Calculation of various molecular properties suggests the compounds to be sufficiently bioavailable.

Coumarin–benzimidazole hybrids were designed, synthesized and evaluated for anti-inflammatory, antioxidant and chronic gastric ulceration potentials. Compounds 4c, 4d and 5a displayed the best anti-inflammatory and antioxidant activities, and proved to be gastric safe.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Acta Pharmaceutica Sinica B - Volume 4, Issue 5, October 2014, Pages 368–375
نویسندگان
, , , ,