Synthesis, Characterization of Ethyl 5-(substituted)-1H-pyrazole- 3-carboxylate Derivative as Potent Anti-inflammatory Agents

Pratik, K Talpara; Arun, K G; Srivastava, Neha; Yogi, Bhumika; Anshuman, Sinha; Kumar, Gupta Sujeet

doi:10.2174/1871523017666180411155240

Cited by 11 publications

(3 citation statements)

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“…However only compound 3 with methoxy substitution at para and meta position exhibited the maximum activity with 54.42 % when compared with diclofenac with 57.88 % inhibition. [41] The above literatures prove that electron withdrawing groups at the phenyl ring of pyrazole contributes towards COX-2 inhibitory as well anticancer activity.…”

Section: 5-diaryl Pyrazolesmentioning

confidence: 94%

“…Ten ethyl 5‐(substituted)‐1H‐pyrazole‐3‐carboxylate bearing substitutions like phenyl, methoxy, dimethoxy, nitro and hydroxyl were evaluated for anti‐inflammatory activity using carrageenan‐induced rat paw edema method. However only compound 3 with methoxy substitution at para and meta position exhibited the maximum activity with 54.42 % when compared with diclofenac with 57.88 % inhibition [41] …”

Section: Di‐substituted Pyrazole Derivativesmentioning

confidence: 95%

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Structural Insights into Pyrazoles as Agents against Anti‐inflammatory and Related Disorders

et al. 2022

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Pyrazole moiety is considered as the most important therapeutic agent for the treatment of inflammation and inflammation associated cancers. Celecoxib, Ramifenazone, Rimonabant and Lonazolac are some of the commercially available pyrazole moieties which are potent COX‐2 inhibitors and also acts in inhibiting various cancers. Recently there are numerous reviews on the biological significance of pyrazole derivatives. However, this review discusses pyrazole derivatives possessing anti‐inflammatory and anticancer activity (COX inhibition) and also illustrates the recent updates on pyrazole research emphasizing on the medicinal chemistry aspects such as the key structural fragments required for the biological activity. There are series of pyrazoles like di‐substituted, tri‐substituted, tetra‐substituted pyrazoles, pyrazole hydrazones, pyrazoles bearing various other heterocycles, bicyclic fused pyrazoles, tricyclic fused pyrazoles, and miscellaneous class of pyrazoles. All these pyrazoles are being researched as COX inhibitors, anti‐inflammatory and against related disorders like cancer.

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Section: 5-diaryl Pyrazolesmentioning

confidence: 94%

Section: Di‐substituted Pyrazole Derivativesmentioning

confidence: 95%

Structural Insights into Pyrazoles as Agents against Anti‐inflammatory and Related Disorders

et al. 2022

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“…Inflammation is an essential defense and survivorship mechanism against harmful stimuli and bodily injuries [1,2]. The inflammatory process involves complex responses from a variety of mediators capable of eliciting heat, flushing, edema, pain, or loss of function of the inflamed tissues [3–5].…”

Section: Introductionmentioning

confidence: 99%

Development of pyrazole derivatives in the management of inflammation

Turones

Martins

Moreira

et al. 2020

Fundamemntal Clinical Pharma

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The therapeutic limitations and poor management of inflammatory conditions are anticipated to impact patients negatively over the coming decades. Following the synthesis of the first pyrazole—antipyrine in 1887, several other derivatives have been screened for anti‐inflammatory, analgesic, and antipyretic activities. Arguably, the pyrazole ring, as a major pharmacophore and central scaffold partly, defines the pharmacological profile of several derivatives. In this review, we explore the structural–activity relationship that accounts for the pharmacological profile of pyrazole derivatives and highlights future research perspectives capable of optimizing current advancement in the search for safe and efficacy anti‐inflammatory drugs. The flourishing research into the pyrazole derivatives as drug candidates has advanced our understanding of inflammation‐related diseases and treatment.

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Therapeutic management of arthritis: A review on structural and target‐based approaches

Mahore

Kamboj

Kaleem

et al. 2022

Archiv der Pharmazie

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Inflammation is the natural defense mechanism against any external stimuli in the human body and it saves us from foreign entities that may alter our bodies' normal functioning. Any anomaly in this natural defense system leads to the development of different pathological conditions associated with chronic inflammation like rheumatoid arthritis, osteoarthritis, atopy, asthma, allergic rhino-conjunctivitis, coronary artery disease, cardiac arrhythmias, obesity, insulin resistance and type-2 diabetes, depression, and aging. These disorders impair the quality of life of affected people in different ways. Among these, rheumatoid arthritis and osteoarthritis are the most common chronic inflammation-associated disorders. Different therapeutic strategies are already available for the treatment of rheumatoid arthritis and osteoarthritis, but all with pros and cons. Here, we discuss the emergence of several antiarthritic analogs developed by different researchers which could provide the basis for the evolution of newer therapeutic strategies with better activity and safety profiles.

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Synthesis, Characterization of Ethyl 5-(substituted)-1H-pyrazole- 3-carboxylate Derivative as Potent Anti-inflammatory Agents

Abstract: The results of the current study indicate that the substitution at pyrazole scaffold could improve anti-inflammatory activity.

Cited by 11 publications

References 0 publications

Structural Insights into Pyrazoles as Agents against Anti‐inflammatory and Related Disorders

Structural Insights into Pyrazoles as Agents against Anti‐inflammatory and Related Disorders

Development of pyrazole derivatives in the management of inflammation

Therapeutic management of arthritis: A review on structural and target‐based approaches

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