Preparation of 5-aryl-3-alkylthio-1,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity


Tozkoparan B. , KUPELI E., YESILADA E., Ertan M.

BIOORGANIC & MEDICINAL CHEMISTRY, cilt.15, ss.1808-1814, 2007 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 15 Konu: 4
  • Basım Tarihi: 2007
  • Doi Numarası: 10.1016/j.bmc.2006.11.029
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY
  • Sayfa Sayıları: ss.1808-1814

Özet

In this study, a series of 5-aryl-3-alkylthio-1,2,4-triazoles and corresponding sulfones were prepared with the objective of developing better analgesic-antiinflammatory compounds with minimum ulcerogenic risk. The structures of the compounds were elucidated by spectral and elemental analysis. The compounds were assayed per os in mice for their antiinflammatory and analgesic activity as well as the ulcerogenic risk and acute toxicity. Several of these compounds showed significant activity. Alkylsulfone derivatives were found to be much more potent analgesic-antimflammatory agents than the corresponding alkylthio analogs. Compounds 9 and 11 were the most active of the series in both analgesic and antiinflammatory activity tests. In contrast to reference compound acetyl salicylic acid, these compounds did not induce gastric lesions in the stomach of experimental animals at the doses that exhibited analgesic/antiinflammatory activity. (c) 2006 Elsevier Ltd. All rights reserved.