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- Title
Synthesis of Novel Substituted Thiourea and Benzimidazole Derivatives Containing a Pyrazolone Ring as Anti-Inflammatory Agents.
- Authors
Moneer, Ashraf A.; Mohammed, Khaled O.; El ‐ Nassan, Hala B.
- Abstract
Two series of new 1-(alkyl/aryl)-3-{2-[(5-oxo-4,5-dihydro-1 H-pyrazol-3-yl)amino]phenyl}thioureas 2a- h and 5-[2-(substituted amino)-1 H-benzimidazol-1-yl]-4 H-pyrazol-3-ols 3a- i were designed and synthesized as anti-inflammatory agents. The cyclooxygenase inhibitory activity of the newly synthesized compounds was investigated. All the compounds showed non-selective inhibition of COX-1 and COX-2 enzymes which was consistent with their docking results. Compounds 2c, 2f, 2g, 3b, and 3g that showed the highest COX-2 inhibitory activity were selected for further in vivo testing as anti-inflammatory agents using diclofenac as a reference drug. Two of the test compounds ( 2c and 3b) showed potent anti-inflammatory activity comparable to that of diclofenac with lower ulcerogenic effect relative to indomethacin. SAR study of the two series as cyclooxygenase inhibitors and anti-inflammatory agents was also provided.
- Subjects
CHEMICAL synthesis; THIOUREA; BENZIMIDAZOLE derivatives; PYRAZOLONES; ANTI-inflammatory agents; CYCLOOXYGENASES
- Publication
Chemical Biology & Drug Design, 2016, Vol 87, Issue 5, p784
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12712