Synthesis, anti-inflammatory, antiplatelet and in silico evaluations of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo-3H-benzoxazole-6-yl)-1-phenyl-1H-pyrazole-4-yl)acrylamides

BAYTAŞ S., Dural N. N. T., ÖZKAN Y., Simsek H. B., Gursel T., Unlu S.

TURKISH JOURNAL OF CHEMISTRY, cilt.36, sa.3, ss.367-382, 2012 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 36 Sayı: 3
  • Basım Tarihi: 2012
  • Doi Numarası: 10.3906/kim-1110-8
  • Dergi Adı: TURKISH JOURNAL OF CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, TR DİZİN (ULAKBİM)
  • Sayfa Sayıları: ss.367-382
  • Gazi Üniversitesi Adresli: Evet

Özet

A series of (E)-3-(3-(2,3-dihydro-3-methyl-2-oxo-3H-benzoxazole-6-yl)-1-phenyl-1H-pyrazole-4-yl)acrylamides (7a-k) were synthesized and evaluated for their in vitro inhibitory activities on COX-1 and COX-2 isoforms using a human whole blood assay as well as their antiplatelet profile against human platelet aggregation using arachidonic acid as agonists. Among the synthesized derivatives 7a-k, especially compound 7g exhibited dual anti-inflammatory and antiplatelet activity with selective COX-2 inhibition.