Synthesis of some novel quinazolin-4(3H)-one hybrid molecules as potent urease inhibitors

Mentese E., Akyuz G., Yilmaz F., Baltas N., Emirik M.

ARCHIV DER PHARMAZIE, vol.351, no.12, 2018 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 351 Issue: 12
  • Publication Date: 2018
  • Doi Number: 10.1002/ardp.201800182
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Keywords: coumarin, furan, molecular docking, quinazolin-4(3H)-one, thiadiazole, triazole, urease inhibition, BIOLOGICAL EVALUATION, BENZIMIDAZOLE DERIVATIVES, ANTIOXIDANT ACTIVITIES, COUMARIN DERIVATIVES, ANTI-UREASE, IN-VITRO, QUINAZOLINONE, DOCKING, 1,2,4-TRIAZOLE, BEARING
  • Recep Tayyip Erdoğan University Affiliated: Yes


A new series of quinazolinone hybrid molecules containing coumarin, furan, 1,2,4-triazole and 1,2,4-thiadiazole rings was designed, synthesized, and screened for their urease inhibition activities. All newly synthesized compounds showed outstanding urease inhibitory potentials with IC50 values ranging between 1.26 +/- 0.07 and 7.35 +/- 0.31 mu g/mL. Among the series, coumarin derivatives (10a-d) exhibited the best inhibitory effect against urease in the range of IC50 = 1.26 +/- 0.07 to 1.82 +/- 0.10 mu g/mL, when compared to standard urease inhibitors such as acetohydroxamic acid and thiourea (IC50 = 21.05 +/- 0.96 and 15.08 +/- 0.71 mu g/mL, respectively). Molecular docking studies were also performed to analyze the binding mode of compound 10b, and supported the experimental results.