Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus
New two derivatives of 2- methyl benzoimidazole were designed, synthesized and evaluated as a potential cyclooxygenase-2 [COX-2] inhibitors. The synthesized compounds have been recognized according to their spectral FT-IR, 1H-NMR data and physical pro- perties. The newly synthesized compounds we...
| Main Authors: | , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
College of Pharmacy / Mustansiriyah University
2019-12-01
|
| Series: | Al-Mustansiriyah Journal of Pharmaceutical Sciences |
| Subjects: | |
| Online Access: | https://ajps.uomustansiriyah.edu.iq/index.php/AJPS/article/view/646 |
| Summary: | New two derivatives of 2- methyl benzoimidazole were designed, synthesized and evaluated as a potential cyclooxygenase-2 [COX-2] inhibitors. The synthesized compounds have been recognized according to their spectral FT-IR, 1H-NMR data and physical pro-
perties. The newly synthesized compounds were investigated in vivo for their anti-inflammatory activities using egg-white stimulated paw edema method with respect to the effect of propylene glycol 50%v/v [control group] and the ibuprofen [10mg/kg i.p.] was selected as a reference ligand. New compounds showed a significantly higher in vivo anti-inflammatory activity compared with ibuprofen as a reference drug. COX-2 selectivity evaluation through molecular docking via GOLD suite [v. 5.6.2.]. The new compounds via molecular docking showed significant higher activities when compared with ibuprofen as referenced drugs because of having hydrogen bonding interaction toward the key amino acids within COX-2 structure and all these results were compatible with the study of in vivo acute anti-inflammatory activities for tested compounds. ADME studies were performed to predict absorption, bioavailability, topological polar surface area, and drug-likeness. The results of ADME studies showed that all synthesized compounds absorbed from the gastrointestinal tract.
|
|---|---|
| ISSN: | 1815-0993 2959-183X |