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, cilt.349, ss.741-748, 2016 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 349 Konu: 9
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1002/ardp.201600122
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Sayfa Sayıları: ss.741-748

Özet

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.