Pyrazole Scaffolds: Centrality in Anti-Inflammatory and Antiviral Drug Design

Abstract

Background: Pyrazole is a component of a diversity of bioactive heterocyclic congeners with a broad-spectrum range of biological and pharmacological uses. Designing novel pyrazole and its analogues, revealing new routes for synthesizing this nucleus, exploring various potencies of that heterocycles, and looking for possible applications of pyrazoles are all becoming more important due to their numerous potential applications. Objectives: Pyrazole scaffolds have been proven to be successful as anti-viral and anti-inflammatory therapeutic against multiple targets like HSV-1, NNRTI, H1N1, CoX-1, and CoX-2. Due to this miscellany in the biotic area, this moiety has engrossed the consideration of many scientists to study chemistry and pharmacological profile. Results: The review encompasses pyrazole having various scaffolds with multiple biological activities and attempts have also been made to correlate their structure-activity relationship. Multiple pyrazole correspondents have been synthesized as lead molecules and performed valuation for their actions. Conclusion: The incorporation of pyrazole with other pharmacophores in the molecule might lead to novel potent therapeutic agents that will further help in designing potent lead molecules.

Convenient One‐Pot Synthesis and Biological Evaluation of New 3,5‐Dimethyl‐1H‐pyrazole‐1‐carbothiohydrazide Derivatives as Anti‐Tumor Agents

“…When 3,5-dimethyl-1H-pyrazole-1-carbothiohydrazide (1) was reacted with stearic acid (10), two water molecules are eliminated, resulting in the formation of 2-heptadecyl-5-(3,5dimethyl-1H-pyrazol-1-yl)-1,3,4-thiadiazole (11). Nonetheless, Simino-hydroxybenzothioate derivatives 13 a-c were subsequently produced by removing just one water molecule when chemical 1 was treated with comparable carboxylic acids 12 ac, such as 4-hydroxybenzoic acid, gallic acid, or salicylic acid, as Scheme 3 describes.…”

“…Additionally, they can enhance the polarity and water solubility of the molecules. [5,6] Leading to the development of universal biological traits, such as antibacterial characteristics, [7,8] antimalarial effects, [9] anti-inflammatory traits, [10] antiviral qualities, [11] antitubercular abilities, [12] and anticancer effects. [13,14] Additionally, pyrazole derivatives, in particular, pyrazole hybrids, showed significant anti-tumor capabilities both in vivo and in vitro by triggering apoptosis, regulating autophagy, and interfering with the cell cycle.…”

Small Molecules as Anti‐inflammatory Agents: Molecular Mechanisms and Heterocycles as Inhibitors of Signaling Pathways

“…[135] For example, clinically approved drugs celecoxib for inflammation, CDPPB as an antipsychotic, and difenamizole as an analgesic are well docu-mented in the literature. [136,137] To the date, many pyrazoles have been designed, synthesised and screened for antiinflammatory activity. Recently, Bekhit et al developed more potent, more selective, and less toxic new COX-2 inhibitors with analgesic and anti-inflammatory efficacy.…”

Novel Pyrazole‐Based Benzofuran Derivatives as Anticancer Agents: Synthesis, Biological Evaluation, and Molecular Docking Investigations

“…The resulting mixture was then refluxed for 5h until TLC indicated the end of the reaction. Thereafter, the reaction mixture was cooled down to room temperature, and a solid precipitated out, which was isolated by simple filtration and recrystallized from ethanol to afford pure products (1)(2)(3)(4)(5)(6)(7)(8).…”

“…Pyrazole derivatives are an essential group of heterocyclic ring systems with various pharmacological activities, [3] such as antimicrobial, [4] anti‐inflammatory, [5] antiviral, [6] anti‐Alzheimer, [7] and anticancer agents [8] . Among the major pyrazole‐based antitumor drugs available on the market are Crizotinib and Ruxolitinib (Figure 1), [9] which have provided some hope in the lives of cancer patients.…”