Synthesis and biological evaluation of new nicotinate derivatives as potential anti-inflammatory agents targeting COX-2 enzyme

El-Dash, Yara; Khalil, Nadia A.; Ahmed, Eman M.; Hassan, Marwa S.A.

doi:10.1016/j.bioorg.2020.104610

Cited by 17 publications

(12 citation statements)

References 35 publications

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“…Moreover, compounds 48a and 48b ( Figure 5 ) demonstrated SIs of 1.8–1.9 fold higher than celecoxib. Gastric toxicity and histopathological studies showed that compounds 48a and 48b had no gastric toxicity, which was consistent with their highly selective inhibitory effect of COX-2 enzyme in vitro 63 .…”

Section: Recent Development In Anti-inflammatory Agentssupporting

confidence: 71%

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Bian

Wu³

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Inflammation and disease are closely related. Inflammation can induce various diseases, and diseases can promote inflammatory response, and two possibly induces each other in a bidirectional loop. Inflammation is usually treated using synthetic anti-inflammatory drugs which are associated with several adverse effects hence are not safe for long-term use. Therefore, there is need for anti-inflammatory drugs which are not only effective but also safe. Several researchers have devoted to the research and development of effective anti-inflammatory drugs with little or no side effects. In this review, we studied some small molecules with reported anti-inflammatory activities and hence potential sources of anti-inflammatory agents. The information was retrieved from relevant studies published between January 2019 and May, 2021 for review. This review study was aimed to provide relevant information towards the design and development of effective and safe anti-inflammation agents.

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Section: Recent Development In Anti-inflammatory Agentssupporting

confidence: 71%

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Bian

Wu³

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…Among these, cyclooxygenase (COX) has been identified as a major regulator of non-steroidal anti-inflammatory drugs (NSAIDs)-and H. pylori-induced inflammation. 48 There are two isoforms of COX, including COX1, which is a constitutively expressed enzyme involved in prostaglandin production in many tissues, and COX2, a proinflammatory mediator induced by the H. pylori infection and contributing a role in H. pylori-induced gastritis, as evidenced by studies on selective COX2 inhibitors. 49 On the other hand, COX-1 is highly expressed in normal cells, suggesting a key role for this enzyme in tissue integrity.…”

Section: Anti-inflammatory and Antioxidant Characteristicsmentioning

confidence: 99%

Benzimidazole derivatives: A versatile scaffold for drug development against Helicobacter pylori‐related diseases

Rostami

Haddadi

2022

Fundamemntal Clinical Pharma

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Helicobacter pylori (H. pylori) is a microaerophilic gastric pathogen and a major contributor to chronic atrophic gastritis, peptic ulcer, and gastric malignancies. The increasing prevalence of H. pylori infection and its related diseases, such as gastric cancer (GC), motivates medicinal chemists to seek for more effective multi‐targeting drugs to prevent and treat H. pylori‐related clinical complications. Benzimidazole, a hetero‐aromatic bicyclic ring compound, has claimed a prominent role in medicinal chemistry owing to its broad range of biological activities, including antibacterial, antiviral, antidiabetic, and anticancer activities. Studies highlight the promising therapeutic potential of benzimidazole derivatives in the treatment of H. pylori‐related clinical complications such as gastric infection, gastritis, peptic ulcer, and GC. Accordingly, we here aimed to scrutinize the role of active molecules of benzimidazole derivatives as potential antibacterial, anti‐urease, anti‐inflammatory, anti‐ulcerative, and anticancer agents, which are expected to find their ways to the clinical setting sooner or later. Due to the role of structural moieties in determining the biological behaviors of benzimidazole derivatives, we explored the structure–activity relationship (SAR) of these compounds to further expand the scope of design of and research on new drugs against H. pylori‐related diseases.

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“…Next, we were curious to employ 1,3-dicarbonyl compounds like β-keto esters ( 2y and 2z ) as strong carbonucleophiles in the domino reactions with 1a–1d under solvent-free conditions. Surprisingly, these reactions produced an exciting class 27 of 2,6-disubstituted nicotinates 4ay , 4dy and 4az as major isomers in 84%, 77% and 75% yields, respectively and minor isomers 3ay–3az in negligible conversions (<3–5%, not isolated). Furthermore, while using a cyclic 1,3-dicarbonyl compound 2zz (dimedone), it led to exclusively 7,8-dihydroquinolin-5(6 H )-one 4azz in 81% yield (Scheme 4).…”

Section: Resultsmentioning

confidence: 99%

Regioselective access to di- and trisubstituted pyridines via a metal-oxidant-solvent-free domino reaction involving 3-chloropropiophenones

2022

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Synthesis and biological evaluation of new nicotinate derivatives as potential anti-inflammatory agents targeting COX-2 enzyme

Cited by 17 publications

References 35 publications

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review

Benzimidazole derivatives: A versatile scaffold for drug development against Helicobacter pylori‐related diseases

Regioselective access to di- and trisubstituted pyridines via a metal-oxidant-solvent-free domino reaction involving 3-chloropropiophenones

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