Synthesis and Biological Evaluation of Novel Bischalcone Derivatives as Carbonic Anhydrase Inhibitors
ARCHIV DER PHARMAZIE, cilt.349, sa.9, ss.741-748, 2016 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 349 Sayı: 9
- Basım Tarihi: 2016
- Doi Numarası: 10.1002/ardp.201600122
- Dergi Adı: ARCHIV DER PHARMAZIE
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
- Sayfa Sayıları: ss.741-748
- Anahtar Kelimeler: Bischalcone, Carbonic anhydrase inhibition, Diazotization, Solvent-free, THERAPEUTIC APPLICATIONS, CHALCONE DERIVATIVES, IN-VITRO, DRUGS, CYTOTOXICITY, ACTIVATORS, ANALOGS, DESIGN, ENZYME, SERIES
- Ondokuz Mayıs Üniversitesi Adresli: Evet
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.