Design, synthesis and pharmacological evaluation of novel azole derivatives of aryl acetic acid as anti-inflammatory and analgesic agents

Amir, Mohd; Saifullah, Khalid; Akhter, Wasim

doi:10.3109/14756366.2010.481622

Cited by 12 publications

(6 citation statements)

References 27 publications

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“…It has been also reported that this compound has greater selectivity against COX-2 when compared to COX-1 (22). Other studies reported that substituted 1,3,4-oxadiazole/tiadiazole and 1,2,4 triazole compounds have anti-inflammatory activities (23)(24)(25)(26). Similarly, Sowmya et.…”

Section: Discussionmentioning

confidence: 84%

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

Kaya-Yasar¹,

Barut²,

Engin³

et al. 2020

Acta Poloniae Pharmaceutica - Drug Research

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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.

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Section: Discussionmentioning

confidence: 84%

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

Kaya-Yasar¹,

Barut²,

Engin³

et al. 2020

Acta Poloniae Pharmaceutica - Drug Research

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“…Encouraged by these observations and in the course of our research program on the synthesis of five membered heterocyclic compounds as anti-inflammatory agents 10 , 21 , 22 , 23 , 24 , we report herein the synthesis and evaluation of some new pyrazolyl urea derivatives as potential anti-inflammatory agents.…”

Section: Introductionmentioning

confidence: 94%

Synthesis, characterization and pharmacological evaluation of pyrazolyl urea derivatives as potential anti-inflammatory agents

Somakala

Amir

2017

Acta Pharmaceutica Sinica B

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p38α mitogen activated protein kinase (MAPK) inhibitors provide a novel approach for the treatment of inflammatory disorders. A series of fifteen pyrazolyl urea derivatives (3a—o) were synthesized and evaluated for their p38α MAPK inhibition and antioxidant potential. Compounds 3a—e, 3g and 3h showed low micromolar range potency (IC50 values ranging from 0.037 ± 1.56 to 0.069 ± 0.07 µmol/L) compared to the standard inhibitor SB 203580 (IC50 = 0.043 ± 3.62 µmol/L) when evaluated for p38α MAPK inhibition by an immunosorbent-based assay. Antioxidant activity was measured by a 2,2′-diphenyl-1-picryl hydrazyl radical (DPPH) free radical scavenging method and one of the compounds, 3c, showed better percentage antioxidant activity (75.06%) compared to butylated hydroxy anisole (71.53%) at 1 mmol/L concentration. Compounds 3a—e, 3g and 3h showed promising in vivo anti-inflammatory activity (ranging from 62.25% to 80.93%) in comparison to diclofenac sodium (81.62%). The ulcerogenic liability and lipid peroxidation activity of these compounds were observed to be less in comparison to diclofenac sodium. These compounds also potently inhibited the lipopolysaccharide (LPS)-induced TNF-α release in mice (ID50 of 3a—c = 19.98, 11.32 and 9.67 mg/kg, respectively). Among the screened compounds, derivative 3c was found to be the most potent and its binding mode within the p38α MAPK is also reported.

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“…Tetrazoles and their derivatives can be utilized as a bio-isosteric replacement to carboxylic acids resulting in their all-important and major part of the applications in medicinal chemistry. Many of the tetrazole derivatives are used as anticancer, [2,3] antibacterial, [4,5] anti-inflammatory, [6,7] analgesic, [7] anti-allergic, [8] antifungal, [3,9] antiulcer [10] etc. They have also found herbicide, fungicide, and plant growth regulator applications in agriculture.…”

Section: Introductionmentioning

confidence: 99%

Advances in Tetrazole Synthesis – An Overview

2022

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Most of the active pharmaceutical ingredients (API) contain the tetrazole ring, thus making them of vast significance in new drug design descriptors. With this importance in view, enormous studies are being carried out on the synthesis of tetrazole derivatives. The methods of its synthesis are [3+2] cycloaddition, multicomponent reactions, microwave‐assisted synthesis using heterogeneous and homogeneous catalysts. Hence, it is necessary to highlight the green catalysis that would be more environmentally benign and economically viable. In this review, we discuss the tetrazole synthesis processes carried out in the presence of heterogeneous and homogeneous catalysts. These catalytic materials gave higher product yield in a shorter reaction time and were reusable.

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Design, synthesis and pharmacological evaluation of novel azole derivatives of aryl acetic acid as anti-inflammatory and analgesic agents

Cited by 12 publications

References 27 publications

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

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

Synthesis, characterization and pharmacological evaluation of pyrazolyl urea derivatives as potential anti-inflammatory agents

Advances in Tetrazole Synthesis – An Overview

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