Synthesis of New Coumarin-C<sub>3</sub> Benzimidazole Hybrids and Their Urease Inhibition Studies

Akyüz G., Mentese E.

LETTERS IN ORGANIC CHEMISTRY, vol.20, no.9, pp.864-870, 2023 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 20 Issue: 9
  • Publication Date: 2023
  • Doi Number: 10.2174/1570178620666230418113901
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Chemical Abstracts Core
  • Page Numbers: pp.864-870
  • Keywords: Hybridization, coumarin-benzimidazole hybrids, chlorine atom, urease activity, weatherburn's method, fused hybrids
  • Recep Tayyip Erdoğan University Affiliated: Yes


A novel series of coumarin-benzimidazole hybrids were designed, synthesized, and extensively characterized using spectral data, including FT-IR, 1H-NMR, and 13C-NMR. Weatherburn's method was used to test new compounds' inhibition of urease activity. The results were evaluated by considering the effects of different side groups and hybridization. The chlorine atom in the molecules notably affects the inhibitory activity of urease. The best result was obtained with the compound “6- chloro-N'-{[5,6-dichloro-2-(2-thienylmethyl)-1H-benzimidazol-1-yl]acetyl}-2-oxo-2H-chromene-3- carbohydrazide” (3b) with IC50= 12.48±0.12 μg/mL against Jack bean urease.