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Novel Aryl/Alkyl Azole Derivates as an anti-nociceptive and anti-inflammatory drug candidates

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Kaya-Yasar Y., Barut E. N., Engin S., Dogan I. S., Sezen F. S.

Acta Poloniae Pharmaceutica - Drug Research

2020

vol. 77

issue 2

289-294

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. 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 is 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.

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1 Acta Poloniae Pharmaceutica - Drug Research

1 2020

1 Barut E. N.

1 Dogan I. S.

1 Engin S.

1 Kaya-Yasar Y.

1 Sezen F. S.

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Novel Aryl/Alkyl Azole Derivates as an anti-nociceptive and anti-inflammatory drug candidates