DOI: 10.33483/jfpau.1311157 ISSN:

İMİDAZOLİNON BAZLI SÜLFONAMİD TÜREVLERİ: SENTEZ, KARAKTERİZASYON VE BAZI METABOLİK ENZİMLERE KARŞI İNHİBİTÖR ÖZELLİKLERİ

Mehtap TUĞRAK SAKARYA, Halise İnci GÜL, Cem YAMALI, Yeliz DEMİR, İlhami GÜLÇİN
  • Pharmaceutical Science
  • Pharmacology
Show PDF Cite
Objective: The purpose of the work was to investigate new synthetic compounds of imidazolinone-based sulfonamide derivatives as potent and selective enyzme inhibitors. A number of compounds synthesized and their inhibitory action against acetylcholine esterase (AChE), and human (h) carbonic anhydrase (CA) isoforms I and II were investigated. Material and Method: The identity of the compounds has been confirmed by HRMS, 1H NMR, and 13C NMR. The pharmacological potential of the compounds has been determined by in vitro enzyme-based assays. Result and Discussion: In this study, a series of imidazolinone-based sulfonamide derivatives were synthesized from 4-(2,4-dimethoxybenzylidene)-2-phenyloxazol-5(4H)-one, sodium acetate, glacial acetic acid, and suitable sulfonamide derivatives such as sulfaguanidine (3), sulfanilamide (4), sulfadiazine (5). These compounds showed potent inhibitory action against acetylcholine esterase (AChE), and human (h) carbonic anhydrase (CA) isoforms I and II. Compound 4 (Ki=19.53±1.23 nM) was a potent and selective inhibitor against hCA I while compound 3 (Ki=16.49±2.20 nM) was found to be potent inhibitor against hCA II. Compound 5 with Ki of 11.68±1.45 nM showed a potent inhibitory effect against the AChE enzyme. Imidazolinone-based sulfonamides can be used in the design of selective CAs inhibitors and anti-Alzheimer's compounds for further studies.

More from our Archive