2-Aminobenzimidazole conjugates of NSAIDS: novel compounds with immunomodulatory, anti-inflammatory and antioxidant actions

被引:10
作者
Bansal, Yogita [1 ]
Silakari, Om [1 ]
机构
[1] Punjabi Univ, Dept Pharmaceut Sci & Drug Res, MML, Patiala 147002, Punjab, India
关键词
2-Aminobenzimidazole; NSAIDs; Immunomodulatory; Anti-inflammatory; Antioxidant; Lipinski; Ulcerogenic; SELECTIVE INHIBITORS; DISCOVERY; POTENT; DERIVATIVES; DESIGN; ANTAGONISTS; DRUGS; ASSAY; ITK;
D O I
10.1007/s00044-014-1198-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
2-Aminobenzimidazole (ABZ) and guanidine have immunomodulatory activity, whereas NSAIDs have anti-inflammatory activity. We, therefore, developed several novel ABZ-NSAID conjugate compounds and tested their anti-inflammatory and immunomodulatory activities. We also measured their antioxidant and ulcerogenic properties. We found that all compounds had not only anti-inflammatory activity but they also had immunomodulatory and antioxidant activities. While compound 2 had immunostimulatory activity (humoral antibody titre, HAT 7.2 +/- A 0.20 and carbon clearance index, K 0.030 +/- A 0.001), compound 9 had immunosuppressive activity (HAT 3.4 +/- A 0.24 and K 0.012 +/- A 0.002). These two compounds did not produce ulcers and hence were safe to the gastric mucosa. In addition, we used Lipinski's parameters and found that all compounds had drug-like properties. Thus, we have provided new evidences to use compounds 2 and 9 for the treatment of inflammatory and immunomodulatory disorders like rheumatoid arthritis, ulcerative colitis, multiple sclerosis, osteoarthritis and cancer.
引用
收藏
页码:1170 / 1179
页数:10
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