Synthesis of novel quinazolinone-triheterocyclic hybrides as dual inhibition of urease and ache

MENTEŞE E., Güzel Y. Ü., AKYÜZ G., Karaali N. Ü.

Journal of the Iranian Chemical Society, vol.21, no.9, pp.2425-2431, 2024 (SCI-Expanded, Scopus) identifier identifier

  • Publication Type: Article / Article
  • Volume: 21 Issue: 9
  • Publication Date: 2024
  • Doi Number: 10.1007/s13738-024-03080-0
  • Journal Name: Journal of the Iranian Chemical Society
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
  • Page Numbers: pp.2425-2431
  • Keywords: AChE, Hybride, Inhibition, Quinazolinone, Thiazolidinone, Urease
  • Recep Tayyip Erdoğan University Affiliated: Yes

Abstract

New triheteroyclic compounds containing quinazolinone, thiophene, andthiadiazole /thiazolidinone structureswere synthesized and characterized by FT-IR, 1H–NMR, and13C–NMRspectral data. The new compounds’ inhibitory activities on urease and acetylcholinesterase were assessed. All triheterocyclic compounds with thiadiazole ring have urease and acetylcholinesteraseinhibitory activities.Especially compound 5a; 3-[(5-(phenylamino)-1,3,4-thiadiazol-2-yl]methyl-2-(thiophen-3-ylmethyl)quinazolin-4(3H)-onehas the best urease inhibition result with 13.30 ± 0.15 µg/mL IC50 value, and it also has the best acetylcholinesterase inhibition with 20.30 ± 0.15 µg/mL IC50 value.