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, cilt.21, sa.9, ss.2425-2431, 2024 (SCI-Expanded) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 21 Sayı: 9
  • Basım Tarihi: 2024
  • Doi Numarası: 10.1007/s13738-024-03080-0
  • Dergi Adı: Journal of the Iranian Chemical Society
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
  • Sayfa Sayıları: ss.2425-2431
  • Anahtar Kelimeler: AChE, Hybride, Inhibition, Quinazolinone, Thiazolidinone, Urease
  • Recep Tayyip Erdoğan Üniversitesi Adresli: Evet

Özet

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.