Synthesis and anti-inflammatory activities of novel 5-(3,4-dichlorophenyl)- 3-[(4-substitutedpiperazin-1-yl)methyl]-1,3,4-oxadiaxole-2(3H)-thiones

Koksal M., Yarim M., Erdal A., Bozkurt A.

Drug Research, cilt.64, sa.2, ss.66-72, 2014 (Scopus) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 64 Sayı: 2
  • Basım Tarihi: 2014
  • Doi Numarası: 10.1055/s-0033-1353184
  • Dergi Adı: Drug Research
  • Derginin Tarandığı İndeksler: Scopus
  • Sayfa Sayıları: ss.66-72
  • Anahtar Kelimeler: 1,3,4-oxadiazole-2-thiones, anti-inflammatory drugs, gastric ulceration, piperazine
  • Ondokuz Mayıs Üniversitesi Adresli: Evet

Özet

Purpose: To synthesize a new series of 5-(3,4-dichlorophenyl)-3-[(4- substitutedpiperazin-1-yl)methyl]-1,3,4-oxadiaxole-2-thiones for their anti-inflammatory activity. Methods: The title compounds synthesized by Mannich reaction of prepared 5-(3,4-dichloroÂphenyl)-1,3,4-oxadiazole-2-thione and appropriate substituted piperazine derivatives. The structures of the compounds were confirmed by IR, NMR and elemental analyses. The newly synthesized compounds were evaluated for their anti-inflammatory and ulcerogenic activities. Results: Most of the compounds were found to have significant anti-inflammatory profile in carrageenan footpad edema test. The compounds showed anti-inflammatory activity ranging from 30.6% to 57.8% inhibition. Conclusion: The compounds 5b, 5f, 5i, 5p and 5r showed most prominent anti-inflammatory activity with low gastric ulceration incidence than the reference drug indomethacine. These compounds could serve as lead molecules for further modifications. © Georg Thieme Verlag KG Stuttgart, New York.