Original Article

SYNTHESIS OF 2(3H)-BENZOTHIAZOLINONE DERIVATIVES AS ANALGESIC AND ANTI-INFLAMMATORY AGENTS

  • Yasemin DÜNDAR
  • Bilge ÇAKIR
  • Esra KÜPELI
  • M. Fethi SAHIN

Received Date: 02.12.2005 Accepted Date: 26.04.2006 Turk J Pharm Sci 2006;3(2):51-60

Abstract In this study, we have synthesized new 1-(4-(2-oxobenzothiazolin-3-yl)butyl-4-substituted piperazine, 1-(4-(2-oxobenzothiazolin-3-yl)butanoyl-4-substituted piperazine and 3-(4-(2-oxo-1,3-benzothiazol-2(3H)-yl)butyl)-1,3-benzothiazol-2(3H)-one derivatives and screened for their analgesic and anti-inflammatory activities as well as gastric ulceration potential in animals. The chemical structures of these compounds were elucidated by their IR, 1H-NMR spectral data, and elementel analyses. None of the compounds except compound 5b, 5c caused gastric lesions or bleeding in test animals. Compound 6c was found to have the highest analgesic and anti-inflammatory activity among the synthesized compounds. Özet Bu çalismada, yeni 1-(4-(2-oksobenzotiyazolin-3-il) butil-4-sübstitüepiperazin, 1-(4-(2-oksobenzotiyazolin-3-il) butanoil-4-sübstitüepiperazin ve 3-(4-(2-okso-1,3-benzotiyazol-2(3H)-yl)butil)-1,3-benzotiyazol-2(3H)-on türevleri sentezlenmis ve bunlarin analjezik ve antienflamatuvar aktiviteleri ile deney hayvanlarinda gastrik ülser olusturma potansiyelleri incelenmistir. Bilesiklerin kimyasal yapilari IR, 1H-NMR ve elementel analiz verileri ile kanitlanmistir. Bilesik 5b, 5c disinda, hiçbir bilesik gastrik lezyon veya kanamaya neden olmamistir. Bilesik 6c, sentezlenen bilesikler arasinda en yüksek analjezik ve antienflamatuvar aktiviteye sahiptir.

Keywords: 2(3H)-Benzothiazolinone, analgesic and anti-inflammatory activity