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, cilt.351, 2018 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 351 Konu: 12
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1002/ardp.201800182
  • Dergi Adı: ARCHIV DER PHARMAZIE

Özet

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.