Synthesis and biological evaluation of phloroglucinol derivatives possessing -glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity

BURMAOĞLU S., YILMAZ A. B., Taslimi P., Algul Ö., Kilic D., GÜLÇİN İ.

ARCHIV DER PHARMAZIE, cilt.351, sa.2, 2018 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 351 Sayı: 2
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1002/ardp.201700314
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Anahtar Kelimeler: -glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase, phloroglucinol derivatives, ISOENZYMES I, PHENOLIC-COMPOUNDS, ISOZYMES I, ANTIOXIDANT, ESTERASE, IDENTIFICATION, BROMOPHENOLS, PROFILES, ENZYME, LACTOPEROXIDASE
  • Erzincan Binali Yıldırım Üniversitesi Adresli: Hayır

Özet

A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including -glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed K-i values of 1.14-3.92nM against AChE, 0.24-1.64nM against BChE, 6.73-51.10nM against -glycosidase, 1.80-5.10nM against hCA I, and 1.14-5.45nM against hCA II.