Synthesis and Biological Evaluation of Novel Bischalcone Derivatives as Carbonic Anhydrase Inhibitors


ARSLAN T., Celik G. , Celik H., ŞENTÜRK M., YAYLI N. , EKİNCİ D.

ARCHIV DER PHARMAZIE, vol.349, no.9, pp.741-748, 2016 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 349 Issue: 9
  • Publication Date: 2016
  • Doi Number: 10.1002/ardp.201600122
  • Title of Journal : ARCHIV DER PHARMAZIE
  • Page Numbers: pp.741-748

Abstract

Design and synthesis of a new type of bischalcones as an alternative to natural and synthetic bischalcones are reported for the first time. Key steps involved the solvent-free Claisen-Schmidt condensation of chalcones, and the successful first application of the diazotization-diazocoupling reaction in the synthesis of CNNC-linked bischalcones by simple structural modification of p-aminoacetophenone. The structures of all compounds were confirmed by means of FT-IR, H-1 and C-13 NMR, ESI/MS, and elemental analysis. In addition, the newly synthesized compounds were screened for carbonic anhydrase inhibition activities. Almost all bischalcones exhibited moderate-to-good inhibitory activities.