Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors

Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors Publisher

Moghadam ES¹ ; Alsadi AM² ; Talebi M³ ; Amanlou M^{3, 4} ; Stoll R⁵ ; Amini M^{3, 4} ; Abdeljalil R¹

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1. Department of Chemistry, College of Science, Sultan Qaboos University, P.O. Box 36, Muscat, P.C. 123, 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, 1417614411, Iran
4. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
5. Biomolecular NMR, Ruhr University of Bochum, Bochum, D-44780, Germany

Source: Letters in Drug Design and Discovery Published:2024

Abstract

Background: Highly pathogenic bacteria colonize and maintain themselves with the aid of an enzyme called urease. Consequently, inhibiting urease enzymes can be a promising method for preventing ureolytic bacterial infections. Objective: This study aimed at synthesizing and screening a novel series of benzimidazole derivatives. Methods: Nine novel benzimidazole derivatives 10α-Ɣ were synthesized and isolated. Their structures were elucidated by1H-NMR and IR spectroscopic techniques besides HRMS. The urease inhibition activity of these compounds was evaluated using the standard urease enzyme inhibition kit. An MTT assay was performed on the NIH-3T3 cell line to investigate the cytotoxicity profile. Results: All benzimidazoles 10α-Ɣ exhibited higher urease inhibition activity (3.06–4.40 µM) than the reference standards thiourea and hydroxyurea (IC50: 22 and 100 µM, respectively). 10Ɣ-1 and 10α-1 exhibited the best activity with the IC50 values of 3.06 and 3.13 µM, respectively. Investigation of the cyto-toxicity profile of the target compound showed that all 10α-Ɣ have IC50 values higher than 50 µM on the tested cell line. Conclusion: The results showed that synthesized benzimidazole derivatives could be highly effective as urease inhibitors. © 2024 Bentham Science Publishers.

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4. Synthesis, Bioactivity, and Molecular Docking of Benzimidazole-2-Carbamate Derivatives As Potent Α-Glucosidase Inhibitors, Journal of Molecular Structure (2023)

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Mohsen Amini (5)

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Style	Citing Format
MLA	Moghadam ES, et al.. "Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors." Letters in Drug Design and Discovery, vol. 21, no. 2, 2024, pp. 297-304.
APA	Moghadam ES, Alsadi AM, Talebi M, Amanlou M, Stoll R, Amini M, Abdeljalil R (2024). Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors. Letters in Drug Design and Discovery, 21(2), 297-304.
Chicago	Moghadam ES, Alsadi AM, Talebi M, Amanlou M, Stoll R, Amini M, Abdeljalil R. "Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors." Letters in Drug Design and Discovery 21, no. 2 (2024): 297-304.
Harvard	Moghadam ES et al. (2024) 'Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors', Letters in Drug Design and Discovery, 21(2), pp. 297-304.
Vancouver	Moghadam ES, Alsadi AM, Talebi M, Amanlou M, Stoll R, Amini M, et al.. Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors. Letters in Drug Design and Discovery. 2024;21(2):297-304.
BibTex	@article{ author = {Moghadam ES and Alsadi AM and Talebi M and Amanlou M and Stoll R and Amini M and Abdeljalil R}, title = {Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors}, journal = {Letters in Drug Design and Discovery}, volume = {21}, number = {2}, pages = {297-304}, year = {2024} }
RIS	TY - JOUR AU - Moghadam ES AU - Alsadi AM AU - Talebi M AU - Amanlou M AU - Stoll R AU - Amini M AU - Abdeljalil R TI - Novel 5-Fluoro-6-(4-(2-Fluorophenyl)Piperazin-1-Yl)-2-(4-(4-Methylpiperazin-1-Yl)Phenyl)-1H-Benzo[D]Imidazole Derivatives As Promising Urease Inhib-Itors JO - Letters in Drug Design and Discovery VL - 21 IS - 2 SP - 297 EP - 304 PY - 2024 ER -

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