NOVEL ARYL/ALKYL AZOLE DERIVATIVES AS AN ANTI-NOCICEPTIVE AND ANTI-INFLAMMATORY DRUG CANDIDATES


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Kaya-Yasar Y. , BARUT E. N. , ENGİN S. , Dogan İ. S. , Sezen S. F.

ACTA POLONIAE PHARMACEUTICA, vol.77, no.2, pp.289-294, 2020 (Journal Indexed in SCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 77 Issue: 2
  • Publication Date: 2020
  • Doi Number: 10.32383/appdr/118364
  • Title of Journal : ACTA POLONIAE PHARMACEUTICA
  • Page Numbers: pp.289-294
  • Keywords: pain, inflammation, aryl/alkyl azole, COX-LOX, formalin-induced hind paw edema test, hot plate test, ANTIEPILEPTIC DRUGS, INFLAMMATION, PHARMACOLOGY, INHIBITORS, COX-2

Abstract

Novel aryl/alkyl azole derivative compounds C1 and C2 were screened for in vivo anti-nociceptive and anti-inflammatory activities by using the hot plate test and formalin-induced hind paw edema test, respectively. The ability of these compounds to inhibit cyclooxygenase-1/2 (COX-1/2) and 5/15-lipoxygenase (5/15-LOX) were evaluated in vitro by using a colorimetric method. C1 (30 and 50 mg/kg, i.p.) and C2 (3 and 30 mg/kg, i.p.) increased the latency to withdrawal in the hot plate test, indicating an anti-nociceptive activity. C1(30 and 50 mg/kg) and C2 (3,30 and 50 mg) were able to decrease formalin-induced edema, indicating their anti-inflammatory properties. C1 and C2 exhibited inhibitory effects on the activity of COX(1-2) and 15-LOX. However, neither C1 nor C2 showed an inhibitory effect on 5-LOX. This study demonstrates that C1 and C2 have anti-nociceptive and anti-inflammatory activities, that are partially mediated by inhibition of COX and LOX enzymes. Our results suggest that C1 and C2. novel aryl/alkyl azole compounds. could serve as lead compounds to develop novel therapeutic options for the treatment of pain and inflammation.