Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! On (X network) By
New Bioactive Dipiperazine Derivatives; Synthesis, Molecular Docking and Urease Inhibition Study Publisher



Saeedian Moghadam E1, 4 ; Mohammed Alsadi A2 ; Talebi M3 ; Amanlou M3, 4 ; Amini M3, 4 ; Abdeljalil R1
Authors
Show Affiliations
Authors Affiliations
  1. 1. Department of Chemistry, College of Science, Sultan Qaboos University, P.O. Box 36, Muscat, P.C. 123, Oman
  2. 2. Department of Crop Sciences, College of Agricultural and Marine Sciences, Sultan Qaboos University, Muscat, P.C. 123, Oman
  3. 3. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 1417614411, Iran
  4. 4. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, 1417614411, Iran

Source: ChemistrySelect Published:2023


Abstract

The successful colonization and survival of highly pathogenic bacteria are powerfully aided by an enzyme known as urease. As a result, it has been demonstrated that inhibiting urease enzymes is a promising method for preventing ureolytic bacterial infections. Consequently, the development and synthesis of safe and effective urease inhibitors has emerged as an intriguing field of study for medical chemists. In this paper, synthesis and bioactivity of thirteen novel benzimidazole derivatives are reported as strong urease inhibitors. The structure of target compounds was determined through a variety of spectroscopic methods (HRMS, 1H NMR, IR). Intriguingly, the inhibitory activity of all was higher (IC50: 9.49 to 23.50 μM) than hydroxyurea, which represent the standard (IC50: 100 μM). In conclusion, current compounds that have been reported are potent enough to continue bioassays to discover a new drug candidate. © 2023 Wiley-VCH GmbH.