Synthesis and biological evaluation of some dibenzofuran-piperazine derivatives

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YURTTAŞ L., Abu Mohsen U., ÖZKAN Y., Cobanoglu S., LEVENT S., KAPLANCIKLI Z. A.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.31, sa.6, ss.1177-1183, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 31 Sayı: 6
  • Basım Tarihi: 2016
  • Doi Numarası: 10.3109/14756366.2015.1108971
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.1177-1183
  • Anahtar Kelimeler: Anticholinesterase activity, antiplatelet activity, dibenzofuran, piperazine, SULFATED SMALL MOLECULES, ANTIPLATELET THERAPY, BERAPROST SODIUM, INHIBITORS, ACETYLCHOLINESTERASE, PLATELETS, AGGREGATION, THROMBIN, MECHANISMS, DISEASE
  • Gazi Üniversitesi Adresli: Evet

Özet

In the present paper, a novel series of dibenzofuran-piperazine derivatives were synthesized via the treatment of N-(2-methoxy-3-dibenzofuranyl)-2-chloroacetamide with substituted piperazine derivatives. The chemical structures of the compounds were elucidated by H-1 NMR, C-13 NMR, mass spectral data; elemental analysis and HPLC analysis. Each derivative was evaluated for antiplatelet activity and anticholinesterase activity. Compound 2m with 2-furoyl moiety exhibited high percentage inhibition as much as standard drug aspirin on arachidonic acid (AA)-induced platelet aggregation. None of the compounds presented significant inhibitor effect on collagen-induced platelet aggregation. Furthermore, the anticholinesterase activity of the compounds was determined and they did not show promising inhibitor activity compared with standard drug donepezil.