Abstract
Chalcones are known as versatile, innovative and bioactive chemical scaffolds in drug development studies. In this study, a series of poly-methoxylated chalcones (1-8) were synthesized by Claisen-Schmidt condensation under the basic condition and their carbonic anhydrase (CA) I/II and acetylcholinesterase (AChE) inhibitory effects were firstly evaluated in this study. CA isoenzymes I and II were inhibited in nanomolar concentration with Ki values of 8.75±0.64 - 37.64±2.38 nM (hCA I) and 11.47±3.31- 45.97±4.67 nM (hCA II). The compounds inhibited the AChE enzyme in the range of 34.14±20.79 - 53.65±13.25 nM. The compounds 1, 3 and 5 were the best inhibitors against hCA I, hCA II, and AChE, respectively. The bioassay results showed that the compounds can be considered as the main frame to design novel chalcone-based enzyme inhibitors.
Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
