Synthesis and urease inhibition studies of some new quinazolinones

AKYÜZ G.

JOURNAL OF HETEROCYCLIC CHEMISTRY, cilt.58, sa.5, ss.1164-1170, 2021 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 58 Sayı: 5
  • Basım Tarihi: 2021
  • Doi Numarası: 10.1002/jhet.4247
  • Dergi Adı: JOURNAL OF HETEROCYCLIC CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Aquatic Science & Fisheries Abstracts (ASFA), Chemical Abstracts Core, Chimica, EMBASE
  • Sayfa Sayıları: ss.1164-1170
  • Recep Tayyip Erdoğan Üniversitesi Adresli: Evet

Özet

In this study, novel quinazolinones were designed, synthesized, characterized by FT-IR, H-1-NMR, C-13-NMR spectral data, and LC-MS. New compounds inhibitory activities on urease were assessed. All of the compounds exhibited potent urease inhibitory activities. Especially in the synthesized compounds, 2-benzyl-3-({5-[(4-nitrophenyl)amino]-1,3,4-thiadiazol2-yl}methyl)quinazolin-4(3H)-one has the best inhibitory effect against Jack bean urease with IC50 = 3.30 +/- 0.09 mu g/mL. And also, N-(4-nitrophenyl)-2-[(4-oxoquinazolin-3(4H)-yl)acetyl] hydrazinecarbothioamide, N-(4-fluorophenyl)-2-[(4-oxoquinazolin-3(4H)-yl)acetyl] hydrazinecarbothioamide, and 2-benzyl-3-({5-[(4-fluorophenyl)amino]-1,3,4-thiadiazol-2yl} methyl)quinazolin-4(3H)-one have best activities among the synthesized compounds.