Novel coumarin-based acetohydrazide-1,2,3-triazole derivatives as urease enzyme inhibitors: Synthesis, in vitro evaluation, and molecular dynamics simulation studies.

ABSTRACT: Urease enzyme inhibition is a well-established and promising strategy for preventing the harmful effects of ureolytic bacterial infections, particularly those caused by H. pylori. However, acetohydroxamic acid, the only approved urease inhibitor, has limited use due to significant side effects, including teratogenicity and psycho-neurological symptoms. To discover new inhibitors, novel coumarin-based acetohydrazide-1,2,3-triazole derivatives were synthesized and evaluated for their urease inhibitory activity. All tested compounds displayed remarkable anti-urease activity (IC₅₀ = 1.62-16.91 μM) compared to thiourea as reference standard (IC₅₀ = 23.11 ± 1.02 μM). The most potent derivative,(E)-N'-(4-((1-Benzyl-1H-1,2,3-triazol-4-yl)methoxy)benzylidene)-2-((4,7-di

SUBMITTER: Sepehrmansourie H 

PROVIDER: S-EPMC11825259 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature