A new approach for the synthesis of tri-substituted pyrazole propionic acids derivatives: Anti-inflammatory, antimicrobial and molecular docking studies

Gudimani, Parashuram; Hebbar, Nagashree U; Shastri, Samundeeswari L.; Shastri, Lokesh A.; Shettar, Arun Kashivishwanath; Hoskeri, Joy H.; Joshi, Shreenivas; Sunagar, Vinay A.

doi:10.1016/j.molstruc.2023.135405

Cited by 5 publications

(2 citation statements)

References 26 publications

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“…28) exhibited significant activity, while compounds 46g and 46k demonstrated moderate antiinflammatory effects compared to celecoxib. Similarly, Gudimani et al [110] developed an innovative methodology for synthesizing derivatives of trisubstituted pyrazole propionic acid, subsequently assessing their anti-inflammatory efficacy. The newly synthesized pyrazole acid derivatives (47a-f) and pyrazole ester derivatives (48a-f) underwent screening for their antiinflammatory activity against matrix metalloproteinases (MMPs), specifically MMP-2 and MMP-9, utilizing the gelatin zymography method.…”

Section: Molecular Basis Of Pyrazole's Anti-inflammatory Effectsmentioning

confidence: 99%

Path of Pyrazoles from Synthetic Factors to Anti-inflammatory Potential: A Review

Vashisht,

Sethi,

Bansal

et al. 2024

ajc

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Pyrazoles, a class of heterocyclic compounds, have garnered considerable attention in drug development due to their intriguing properties, particularly those containing a pyrazole moiety. Pyrazole, a pivotal chemical in the creation of potent bioactive agents, encompasses five heterocyclic members. The discovery of certain pyrazole compounds exhibiting robust biological activities has spurred interest in this field of inquiry. Heterocyclic compounds incorporating nitrogen and its derivatives have historically served as crucial sources of medicinal compounds. Given that the heterocyclic group constitutes a vast reservoir of organic molecules, its significance in both theoretical and applied chemistry has grown significantly. Extensive literature indicates that researchers have employed diverse synthetic strategies in recent years to produce substituted pyrazole derivatives with promising biological potential as anti-HIV, anti-inflammatory, antitumor and antimicrobial agents. Inflammation, a multifaceted biological response essential for the body’s defense mechanisms, can also contribute to various pathological conditions when dysregulated. Understanding the underlying molecular mechanisms offers a foundation for targeted interventions against inflammatory disorders. These insights fuel ongoing endeavors to discover effective and innovative anti-inflammatory agents with potential therapeutic applications. This review delves into the synthesis and characterization of various pyrazole derivatives, emphasizing structural modifications influencing their anti-inflammatory efficacy. The insights provided herein are invaluable for the rational design and synthesis of novel anti-inflammatory agents. Furthermore, the review concludes with a discussion on future perspectives, underscoring the imperative for further research to optimize the therapeutic potential of pyrazole derivatives as anti-inflammatory agents.

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Section: Molecular Basis Of Pyrazole's Anti-inflammatory Effectsmentioning

confidence: 99%

Path of Pyrazoles from Synthetic Factors to Anti-inflammatory Potential: A Review

Vashisht,

Sethi,

Bansal

et al. 2024

ajc

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“…They are active molecules in medicinal chemistry because they are easy to synthesize, and their chemical structures can be modified at multiple sites. These compounds exhibit a variety of cytoprotective and modulatory functions, which lead to several therapeutic activities such as anticancer effects [31,32], antimicrobial properties [33][34][35], antifungal agents [36,37], and various other functions [38][39][40].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, Molecular Modeling and Biological Evaluation of Novel Pyrazole Benzimidazolone Derivatives as Potent Antioxidants

Adardour,

Ait Lahcen,

Oubahmane

et al. 2023

Pharmaceuticals

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In the present study, we used benzimidazolone as a starting material to efficiently synthesize several hybrid compounds of pyrazole benzimidazolone derivatives by the 1,3-dipolar cycloaddition reaction. These compounds were obtained in average yields and were characterized by NMR (1H and 13C) and HRMS analysis. The antioxidant activity of the synthesized compounds 5(a–c) and 6(a–c) was evaluated using in vitro reduction assays, including ferric reducing antioxidant power (FRAP) and total antioxidant capacity (TAC). The results indicated that products 5c, 6b, and 6c exhibit higher antioxidant activity compared to the reference compounds and showed a remarkable ability to effectively remove the radical at IC50 (14.00 ± 0.14, 12.47± 0.02, and 12.82 ± 0.10 µM, respectively) under the TAC assessment. Conversely, compound 6c showed excellent activity at IC50 (68.97 ± 0.26 µM) in the FRAP assay. We carried out molecular docking and dynamics simulations to investigate the binding mode and stability of 5c, 6b, and 6c in the active site of human Peroxiredoxin 5. An ADMET study was conducted to determine the drug properties of the synthesized compounds.

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Synthesis, antimicrobial activity and molecular docking study of benzyl functionalized benzimidazole silver(I) complexes

Arı,

Şahin,

Üstün

et al. 2023

J Biol Inorg Chem

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A new approach for the synthesis of tri-substituted pyrazole propionic acids derivatives: Anti-inflammatory, antimicrobial and molecular docking studies

Cited by 5 publications

References 26 publications

Path of Pyrazoles from Synthetic Factors to Anti-inflammatory Potential: A Review

Path of Pyrazoles from Synthetic Factors to Anti-inflammatory Potential: A Review

Design, Synthesis, Molecular Modeling and Biological Evaluation of Novel Pyrazole Benzimidazolone Derivatives as Potent Antioxidants

Synthesis, antimicrobial activity and molecular docking study of benzyl functionalized benzimidazole silver(I) complexes

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