Aryl quinolinyl hydrazone derivatives as anti-inflammatory agents that inhibit TLR4 activation in the macrophages

Debnath, Utsab; Mukherjee, Suprabhat; Joardar, Nikhilesh; Babu, Santi P. Sinha; Jana, Kuladip; Misra, Anup Kumar

doi:10.1016/j.ejps.2019.04.016

Cited by 24 publications

(14 citation statements)

References 40 publications

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“…Furthermore, aryl 7-chloroquinolinyl hydrazone (3a-u) is a synthetic anti-inflammatory drug, which can play an anti-inflammatory effect by inhibiting the activation of macrophage downstream inflammatory cytokine secretion pathway after LPS binding to TLR4. Such inhibitors also provide a possible combination regimen for the clinical treatment of COVID-19 patients with severe inflammatory reactions ( Debnath et al, 2019 ).…”

Section: Tlrs Sensing Of Sars-cov-2mentioning

confidence: 99%

Toll-like receptor (TLRs) agonists and antagonists for COVID-19 treatments

Liu

Yang

et al. 2022

Front. Pharmacol.

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Severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) rapidly infects humans and animals which make coronavirus disease 2019 (COVID-19) a grievous epidemic worldwide which broke out in 2020. According to data analysis of the other coronavirus family, for instance severe acute respiratory syndrome SARS coronavirus (SARS-CoV), can provide experience for the mutation of SARS-CoV-2 and the prevention and treatment of COVID-19. Toll-like receptors (TLRs) as a pattern recognition receptor (PRRs), have an indispensable function in identifying the invader even activate the innate immune system. It is possible for organism to activate different TLR pathways which leads to secretion of proinflammatory cytokines such as Interleukin 1 (IL-1), Interleukin 6 (IL-6), Tumor necrosis factor α (TNFα) and type Ⅰ interferon. As a component of non-specific immunity, TLRs pathway may participate in the SARS-CoV-2 pathogenic processes, due to previous works have proved that TLRs are involved in the invasion and infection of SARS-CoV and MERS to varying degrees. Different TLR, such as TLR2, TLR4, TLR7, TLR8 and TLR9 probably have a double-sided in COVID-19 infection. Therefore, it is of great significance for a correctly acknowledging how TLR take part in the SARS-CoV-2 pathogenic processes, which will be the development of treatment and prevention strategies.

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Section: Tlrs Sensing Of Sars-cov-2mentioning

confidence: 99%

Toll-like receptor (TLRs) agonists and antagonists for COVID-19 treatments

Liu

Yang

et al. 2022

Front. Pharmacol.

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“…synthesised a series of aryl 7-chloroquinolinyl hydrazone derivatives and evaluated their anti-inflammatory activities based on their ability to inhibit secretion of pro-inflammatory cytokines from the macrophages after stimulation with LPS. It was found that compound 62 ( Figure 8 ) was the most promising lead with IC 50 =12.39 ± 0.97 µM 77 .…”

Section: Recent Development In Anti-inflammatory Agentsmentioning

confidence: 99%

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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“…As an example; TAK-242 (resatorvid), a cyclohexane derivative that binds to the SH 2 group of cysteine of the TIR domain. A previously reported compound T5342126 ( Figure 2 ), as a selective TLR4 inhibitor was found to be an inhibitor of the interaction interface of TLR4-MD2 61 , 87–91 . Molecular docking was performed and revealed that the benzyl group of this compound binds with the hydrophobic pocket of TLR4, and the carbazole group occupies the MD2 pocket.…”

Section: Discussionmentioning

confidence: 82%

“…The determination of the cytotoxic effect of our active antioxidant compounds on normal macrophages was critical, as shown in previous studies, many bioactive compounds were reported as toxic agents to normal cells and could be responsible for cells death by disrupting protein synthesis 48–50 , 61 . Table 2 shows the possible cytotoxic activity of our active compounds against macrophage cell line RAW 264.7.…”

Section: Resultsmentioning

confidence: 90%

Novel pyrrolopyrimidine derivatives: design, synthesis, molecular docking, molecular simulations and biological evaluations as antioxidant and anti-inflammatory agents

Sayed

Mansour

Ali

et al. 2022

Journal of Enzyme Inhibition and Medicinal Chemistry

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Current medical approaches to control the Covid-19 pandemic are either to directly target the SARS-CoV-2 via innovate a defined drug and a safe vaccine or indirectly target the medical complications of the virus. One of the indirect strategies for fighting this virus has been mainly dependent on using anti‐inflammatory drugs to control cytokines storm responsible for severe health complications. We revealed the discovery of novel fused pyrrolopyrimidine derivatives as promising antioxidant and anti-inflammatory agents. The newly synthesised compounds were evaluated for their in vitro anti-inflammatory activity using RAW264.7 cells after stimulation with lipopolysaccharides (LPS). The results revealed that 3a, 4b, and 8e were the most potent analogues. Molecular docking and simulations of these compounds against COX-2, TLR-2 and TLR-4 respectively was performed. The former results were in line with the biological data and proved that 3a, 4b and 8e have potential antioxidant and anti-inflammatory effects.

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Aryl quinolinyl hydrazone derivatives as anti-inflammatory agents that inhibit TLR4 activation in the macrophages

Cited by 24 publications

References 40 publications

Toll-like receptor (TLRs) agonists and antagonists for COVID-19 treatments

Toll-like receptor (TLRs) agonists and antagonists for COVID-19 treatments

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

Novel pyrrolopyrimidine derivatives: design, synthesis, molecular docking, molecular simulations and biological evaluations as antioxidant and anti-inflammatory agents

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