期刊
MEDICINAL CHEMISTRY RESEARCH
卷 24, 期 3, 页码 1170-1179出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-014-1198-3
关键词
2-Aminobenzimidazole; NSAIDs; Immunomodulatory; Anti-inflammatory; Antioxidant; Lipinski; Ulcerogenic
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.
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