Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors

Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors Publisher

Saeedian Moghadam E¹ ; Alsadi AM² ; Talebi M^{3, 4} ; Amanlou M³ ; Amini M^{3, 4} ; Abdeljalil R¹

Show Affiliations

1. Department of Chemistry, College of Science, Sultan Qaboos University, Muscat, Oman
2. Department of Crop Sciences, College of Agricultural and Marine Sciences, Sultan Qaboos University, Muscat, Oman
3. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
4. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran

Source: Synthetic Communications Published:2022

Abstract

Herein, we synthesized a series of novel benzimidazole derivatives 5a–k and screened their bioactivity as potent urease inhibitors. The structure of the 5a–k was elucidated using spectroscopic technics (1H-NMR, 13C-NMR, MS), elemental analysis, and melting point. The urease inhibition activity was evaluated using the urease enzyme inhibition kit. All 5a–k, except 5d, showed higher urease inhibition activity (0.77 to 6.25 µM) in comparison to thiourea and hydroxyurea as standard (IC50: 22 and 100 µM respectively). 5c and 5j exhibited the best activity with the IC50 value of 0.77 and 1.26 µM respectively. A molecular docking study showed the mode of interactions between the most active compound and enzyme active site. To investigate the cytotoxicity profile of the target compounds, an MTT assay was done on two different cell lines which showed all 5a–k have IC50 values higher than 50 µM on both tested cell lines. © 2021 Taylor & Francis Group, LLC.

Style	Citing Format
MLA	Saeedian Moghadam E, et al.. "Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors." Synthetic Communications, vol. 52, no. 1, 2022, pp. 106-116.
APA	Saeedian Moghadam E, Alsadi AM, Talebi M, Amanlou M, Amini M, Abdeljalil R (2022). Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors. Synthetic Communications, 52(1), 106-116.
Chicago	Saeedian Moghadam E, Alsadi AM, Talebi M, Amanlou M, Amini M, Abdeljalil R. "Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors." Synthetic Communications 52, no. 1 (2022): 106-116.
Harvard	Saeedian Moghadam E et al. (2022) 'Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors', Synthetic Communications, 52(1), pp. 106-116.
Vancouver	Saeedian Moghadam E, Alsadi AM, Talebi M, Amanlou M, Amini M, Abdeljalil R. Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors. Synthetic Communications. 2022;52(1):106-116.
BibTex	@article{ author = {Saeedian Moghadam E and Alsadi AM and Talebi M and Amanlou M and Amini M and Abdeljalil R}, title = {Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors}, journal = {Synthetic Communications}, volume = {52}, number = {1}, pages = {106-116}, year = {2022} }
RIS	TY - JOUR AU - Saeedian Moghadam E AU - Alsadi AM AU - Talebi M AU - Amanlou M AU - Amini M AU - Abdeljalil R TI - Design, Synthesis, and Bioactivity Investigation of Novel Benzimidazole Derivatives As Potent Urease Inhibitors JO - Synthetic Communications VL - 52 IS - 1 SP - 106 EP - 116 PY - 2022 ER -

Science Communicator Platform

Authors

Authors Affiliations

Abstract