Synthesis and biological evaluation of benzimidazolone bridged triheterocyclic compounds


MENTEŞE E., Guven O., Caliskan N., BALTAŞ N.

JOURNAL OF HETEROCYCLIC CHEMISTRY, cilt.58, sa.6, ss.1259-1267, 2021 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 58 Sayı: 6
  • Basım Tarihi: 2021
  • Doi Numarası: 10.1002/jhet.4252
  • 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.1259-1267
  • Anahtar Kelimeler: acetylcholinesterase inhibition, benzimidazolone, thiosemicarbazide, triazole, urease inhibition, &#945, &#8208, glucosidase inhibition, DERIVATIVES, INHIBITORS, DISCOVERY
  • Recep Tayyip Erdoğan Üniversitesi Adresli: Evet

Özet

A new series of benzimidazolone bridged triheterocyclic compounds bearing thiosemicarbazide, thiadiazole, triazole, moieties was synthesized and then screened for their in vitro urease, alpha-glucosidase, and acetylcholinesterase inhibition properties for the first time. All the synthesized compounds showed an outstanding urease inhibitory effect when compared with standards. Compounds 1, 4, 5b, 5d, 6b, 6d, 7b, and 7d showed significant acetylcholinesterase inhibitory activity with IC50 values between 7.32 +/- 0.58 and 12.52 +/- 0.13 mu g/ml comparable to donepezil (15.12 +/- 0.20 mu g/ml). Compound 5c, having thiosemicarbazide moiety at the positions N-1 and N-3 of benzimidazolone nucleus, showed the highest alpha-glucosidase inhibitory activity (IC50 = 11.42 +/- 0.11 mu g/ml).