Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus

  • Abdul Muhaimen Amjed Adnan Department of Pharmacy, Baghdad College of Medical Science, Baghdad, Iraq.
  • Monther Faisal Mahdi Department of pharmaceutical Chemistry, Ashur University College, Baghdad, Iraq
  • Ayad kareem Khan Department of pharmaceutical Chemistry, College of Pharmacy, University of Mustansiriyah, Baghdad, Iraq.

Abstract

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.


 

Published
2019-12-01
How to Cite
ADNAN, Abdul Muhaimen Amjed; MAHDI, Monther Faisal; KHAN, Ayad kareem. Design, Synthesis, and Acute Anti-inflammatory Assessment of New 2-methyl Benzoimidazole Derivatives Having 4-Thiazolidinone Nucleus. Al-Mustansiriyah Journal of Pharmaceutical Sciences (AJPS), [S.l.], v. 19, n. 4, p. 151-160, dec. 2019. ISSN 1815-0993. Available at: <http://ajps.uomustansiriyah.edu.iq/index.php/AJPS/article/view/646>. Date accessed: 26 may 2020.