216596-59-7Relevant academic research and scientific papers
Synthesis of some novel quinazolin-4(3H)-one hybrid molecules as potent urease inhibitors
Mente?e, Emre,Akyüz, Gülay,Y?lmaz, Fatih,Balta?, Nimet,Emirik, Mustafa
, (2018)
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 μg/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 μg/mL, when compared to standard urease inhibitors such as acetohydroxamic acid and thiourea (IC50 = 21.05 ± 0.96 and 15.08 ± 0.71 μg/mL, respectively). Molecular docking studies were also performed to analyze the binding mode of compound 10b, and supported the experimental results.
