Synthesis and analgesic and anti-inflammatory activity of some new (6-acyl-2-benzoxazolinone and 6-acyl-2-benzothiazolinone derivatives with acetic acid and propanoic acid residues


Unlu S., Onkol T., Dundar Y. , Okcelik B., Kupeli E., Yesilada E., ...Daha Fazla

ARCHIV DER PHARMAZIE, cilt.336, ss.353-360, 2003 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 336 Konu: 8
  • Basım Tarihi: 2003
  • Doi Numarası: 10.1002/ardp.200300746
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Sayfa Sayıları: ss.353-360

Özet

In this study for developing potent analgesic and anti-inflammatory compounds, we synthesized 6-acyl-2-benzoxazolinone and 6-acyl-2-benzothiazolinone derivatives with acetic acid and propanoic acid side chain, and performed preliminary screening of their in vivo analgesic and anti-inflammatory activities at a single dose of 100 mg/kg in mice by a p-benzoquinone-induced writhing test and a Carrageenan-induced hind paw edema model, respectively. We also determined their gastric ulceration effects in the tested animals. Propanoic acid derivatives were generally found to have higher analgesic and anti-inflammatory activities, and among them, 3-(6-benzoyl-2-benzothiazolinon-3-yl)propanoic acid (Compound 4a) exhibited the highest analgesic and anti-inflammatory activity. However, all compounds showed lower anti-inflammatory effects than we observed for indomethacin at 10 mg/kg dose. Consequently, 6-acyl-2-benzoxazolinone/2-benzothiazolinones having propanoic acid side chain might lead to further studies for developing better candidates with potent analgesic and anti-inflammatory effects while acetic acid derivatives do not exhibit comparable satisfactory features.