New Bioactive Dipiperazine Derivatives; Synthesis, Molecular Docking and Urease Inhibition Study

Ebrahim Saeedian Moghadam, Abdullah Mohammed Al-Sadi, Meysam Talebi, Massoud Amanlou, Mohsen Amini*, Raid Abdel-Jalil*

*المؤلف المقابل لهذا العمل

نتاج البحث: المساهمة في مجلةArticleمراجعة النظراء

ملخص

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.

اللغة الأصليةEnglish
رقم المقالe202300124
دوريةChemistrySelect
مستوى الصوت8
رقم الإصدار17
المعرِّفات الرقمية للأشياء
حالة النشرPublished - مايو 5 2023
منشور خارجيًانعم

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