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

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.

Alpha‐lipoic acid: A promising adjuvant for nonsteroidal anti‐inflammatory drugs therapy with improved efficacy and gastroprotection

“…All animals were fasted 18 h before the administration of drugs to ensure gastric emptying. After fasting period, mice were treated with vehicle or different doses of Indo and ALA. To evaluate the antiinflammatory effect, formalin-induced paw edema test was perfomed as described in our previous studies with slight modifications (Barut et al, 2019;Kaya-Yasar et al, 2020). Briefly, 1 h after the vehicle, Indo or ALA administration, the paw thickness and volume were measured with micrometer caliper and plethysmometer (baseline) and 20 μl of freshly prepared 2% formalin solution was injected into plantar surface of the hind paws of the mice to form edema.…”