New 2-Methyl Benzimidazole derivatives bearing 4-Thiazolidinone heterocyclic rings: Synthesis, Preliminary pharmacological assessment and docking studies Adnan Abdul Muhaimen Amjed1, Mahdi Monther Faisal2, Khan Ayad Kareem2* 1Department of Pharmacy, Baghdad College of Medical Science, Baghdad, Iraq 2Department of Pharmaceutical Chemistry, College of Pharmacy, Mustansiriyah University, Baghdad-Iraq *Corresponding Author E-mail: ayad@uomustansiriyah.edu.iq
Online published on 30 April, 2021. Abstract New 2-methyl benzimidazole derivatives were prepared and evaluated as possible inhibitor agents for cyclooxygenase-2 (COX-2). The synthesized derivatives structures have been recognized according to their spectral FT-IR, 1H-NMR data and physical properties. The newly synthesized compounds were inspected in vivo for their anti-inflammation efficiency using egg-white stimulated edema of paw method regarding the effect of propylene glycol 50%v/v as a control group. Ibuprofen (10mg/kg i.p.) was chosen as a reference ligand. New compounds exhibit a significant in vivo anti-inflammatory efficacy approached with ibuprofen as a reference drug. Selective evaluation of cyclooxygenase-2 by stimulating molecular cohesion through (GOLD suite v.5.6.2). All the investigated compounds via molecular docking showed significant more activities comparable with diclofenac and ibuprofen as referenced drugs. ADME studies were performed to estimate site of absorption, bioavailability, topological polar surface area and drug-likeness and it appeared that all synthesized compounds absorbed from GIT. Top Keywords 2-methyl benzimidazole, 4-thiazolidinone, Synthesis, Pharmacological assessment, Docking. Top |