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Synthesis,characterization and pharmacological evaluation of pyrazolyl urea derivatives as potential anti-inflammatory agents

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Acta Pharmaceutica Sinica B 2017年第2期7卷 230-240页

作者： Kanagasabai Somakala Mohammad Amir Department of Pharmaceutical Chemistry Faculty of PharmacyHamdard UniversityNew Delhi 110062India

p38α mitogen activated protein kinase(MAPK) inhibitors provide a novel approach for the treatment of inflammatory disorders.A series of fifteen pyrazolyl urea derivatives(3a-o) were synthesized and evaluated for their p38α MAPK inhibition and antioxidant *** 3a-e,3g and 3h showed low micromolar range potency(IC_(50) values ranging from 0.037 ±1.56 to 0.069± 0.07μmol/L)compared to the standard inhibitor SB 203580(IC_(50) = 0.043 + 3.62μmol/L) when evaluated for p38αMAPK inhibition by an immunosorbent-based *** activity was measured by a 2,2'-diphenyl-1-picryl hydrazyl radical(DPPH) free radical scavenging method and one of the compounds,3c,showed better percentage antioxidant activity(75.06%) compared to butylated hydroxy anisole(71.53%)at 1 mmol/L *** 3a-e,3g and 3h showed promising in vivo anti-inflammatory activity(ranging from 62.25%to 80.93%) in comparison to diclofenac sodium(81.62%).The ulcerogenic liability and lipid peroxidation activity of these compounds were observed to be less in comparison to diclofenac *** compounds also potently inhibited the lipopolysaccharide(LPS)-induced TNF-αrelease in mice(ID_(50) of 3a-c = 19.98,11.32 and 9.67 mg/kg,respectively).Among the screened compounds,derivative 3c was found to be the most potent and its binding mode within the p38α MAPK is also reported.

关键词： Pyrazolyl urea p38 MAPK DPPH Anti-inflammatory gastric toxicity Lipid peroxidation

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Novel coumarin–benzimidazole derivatives as antioxidants and safer anti-inflammatory agents

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Acta Pharmaceutica Sinica B 2014年第5期4卷 368-375页

作者： Radha Krishan Arora Navneet Kaur Yogita Bansal Gulshan Bansal Department of Pharmaceutical Sciences and Drug Research Punjabi UniversityPatiala 147002India

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 *** resultant compounds are expected to exhibit both anti-inflammatory and antioxidant activities along with less gastric toxicity *** series of coumarin–benzimidazole derivatives(4a–e and 5a–e)were synthesized and evaluated for anti-inflammatory activity and antioxidant *** 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(IC_(50) of 19.7,13.9 and 1.2 mmol/L,respectively,versus 23.4 mmol/L for butylatedhydroxytoluene)*** 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 *** of various molecular properties suggests the compounds to be sufficiently bioavailable.

关键词： Anti-inflammatory Benzimidazoles Coumarins DPPH gastric toxicity

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