Novel Oxazolidinone Antibacterial Analogues with a Substituted Ligustrazine C‐ring Unit

Chen, Yan; Ruan, Zhixiong; Wang, Fang; Huangfu, De-Sheng; Sun, Ping‐Hua; Lin, Jing; Chen, Weimin

doi:10.1111/cbdd.12537

Cited by 13 publications

(9 citation statements)

References 44 publications

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“…Therefore, that study concluded that LZD suppresses the production of TNF-α and IFN-γ without exerting any inhibitory effect on endotoxin production by bacteria (Takahashi et al, 2010). (Chen et al, 2015) compared the effects of a series of novel oxazolidinone compounds and LZD on the production of inflammatory mediators (NO, IL-6, and TNF-α) in LPS-stimulated murine macrophages. They found that some of these oxazolidinone compounds exhibited a more significant inhibitory effect than LZD.…”

Section: Introductionmentioning

confidence: 99%

Linezolid and Its Immunomodulatory Effect: In Vitro and In Vivo Evidence

et al. 2019

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Recent studies have explored the effects of some antibacterial agents on various aspects of the immune response to infection in addition to their bactericidal effects. As a synthetic oxazolidinone class of antibacterial agent, linezolid (LZD) exhibits activity against a broad range of Gram-positive bacteria. In the present review, we summarized the effects of LZD on the immune response and new approaches that can exploit such interactions for the treatment of bacterial infections. In vitro and pre-clinical evidence demonstrate that LZD suppresses the phagocytic ability, cytokine synthesis, and secretion of immune cells as well as the expressions of immune-related genes at the mRNA level under the stimulation of endotoxin or pathogens. Immunomodulatory effects of LZD can not only reduce the inflammatory damage induced by exaggerated or prolonged release of pro-inflammatory cytokines during infections but can also be applied to alleviate the symptoms of non-infectious inflammatory conditions. Further research is necessary to explore the molecular mechanisms involved and confirm these findings in clinical practice.

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Section: Introductionmentioning

confidence: 99%

Linezolid and Its Immunomodulatory Effect: In Vitro and In Vivo Evidence

et al. 2019

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“…Recent studies showed that natural products or herbal components provide a new direction for drug research and development . Tetramethylpyrazine (TMP), an effective blood circulation drugs, exhibits an ample array of pharmacological activities such as antithrombotic , antiangina and antibacterial properties . We previously reported that TMP alleviated carbon tetrachloride (CCl 4 )‐induced liver fibrosis in vivo and inhibited platelet‐derived growth factor‐β receptor (PDGF‐βR) pathway and NLRP3 inflammasome expression of hepatic stellate cells (HSCs) in vitro .…”

Section: Introductionmentioning

confidence: 99%

Tetramethylpyrazine attenuates sinusoidal angiogenesis via inhibition of hedgehog signaling in liver fibrosis

et al. 2017

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Accumulating evidence indicates that hedgehog signaling plays a pivotal role in pathological angiogenesis and is involved in wound-healing responses in a number of adult tissues, including the liver. We previously demonstrated that hedgehog signaling promoted proliferation and inhibited apoptosis in hepatic stellate cells. This study was aimed to evaluate the effect of tetramethylpyrazine (TMP) on hedgehog signaling and to further examine the molecular mechanisms of TMP-induced antiangiogenesic effects in liver fibrosis. We found that TMP ameliorated the expression of proangiogenic markers vascular endothelial growth factor A (VEGF-A), vascular endothelial growth factor receptor 2 (VEGF-R2), platelet-derived growth factor BB (PDGF-BB), platelet-derived growth factor-β receptor (PDGF-βR) and hypoxia inducible factor 1α (HIF-1α), concomitant with reduced abundance of endothelial markers platelet endothelial cell adhesion molecule-1 (PECAM-1/CD31), CD34 and von willebrand factor in vivo and in vitro. Interestingly, TMP attenuated the abundance of sonic hedgehog, smoothened (Smo) and glioblastoma but increased the expression of hedgehog-interacting protein in liver sinusoidal endothelial cells, which was underlying mechanism for the antiangiogenesic activity of TMP. Downregulation of Smo activity, using selective Smo inhibitor cyclopamine, lead to a synergistic effect with TMP, whereas Smo overexpression plasmid impaired the induction of antiangiogenesic effects of TMP. Overall, these results provide novel implications to reveal the molecular mechanism of TMP-inhibited liver sinusoidal angiogenesis, by which points to the possibility of using TMP-based antiangiogenic drugs for the treatment of liver fibrosis. © 2017 IUBMB Life, 69(2):115-127, 2017.

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“…3,5,6‐Trimethylpyrazine‐2‐carboxylic acid and 2‐(bromomethyl)‐3,5,6‐trimethylpyrazine were prepared from tetramethylpyrazine (Ligustrazine). Details can be found in the reported method (Chen et al., 2015; Wang et al., 2019).…”

Section: Methodsmentioning

confidence: 99%

Design, synthesis, and biological evaluation of benzo[b]thiophene 1,1‐dioxide derivatives as potent STAT3 inhibitors

Wang

et al. 2021

Chem Biol Drug Des

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Signal transducer and activator of transcription (STAT) family consist of seven members, STAT1, 2, 3, 4, 5α, 5β, 6 (Darnell, 1997). Among them, STAT1, STAT3, and STAT5 are highly associated with human tumorigenesis and development due to their frequent hyperactivation (Benekli et al., 2009). In normal cells, STAT3 responds to the stimulation of various extracellular signaling factors and then transmits them through phosphorylation of the tyrosine kinase site (Tyr705) in the SH2 domain. Once in the nucleus, STAT3 binds to DNA and subsequently activates transcription and translation, thus performing various physiological functions (Furtek et al., 2016;Ren et al., 2015;Yamamoto et al., 2002). However, according to previous research, STAT3 is involved in the process of growth, proliferation, angiogenesis, and invasion of tumor cells (Bromberg & Chen, 2001). Abnormally high expression

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Novel Oxazolidinone Antibacterial Analogues with a Substituted Ligustrazine C‐ring Unit

Cited by 13 publications

References 44 publications

Linezolid and Its Immunomodulatory Effect: In Vitro and In Vivo Evidence

Linezolid and Its Immunomodulatory Effect: In Vitro and In Vivo Evidence

Tetramethylpyrazine attenuates sinusoidal angiogenesis via inhibition of hedgehog signaling in liver fibrosis

Design, synthesis, and biological evaluation of benzo[b]thiophene 1,1‐dioxide derivatives as potent STAT3 inhibitors

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