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  2. Design, synthesis and bioactivity evaluation of cinnamic acid derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury

Design, synthesis and bioactivity evaluation of cinnamic acid derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury

  • Bioorg Med Chem Lett. 2025 Feb 1:116:130036. doi: 10.1016/j.bmcl.2024.130036.
Pengqin Chen 1 Pan Chen 2 Xiemin Wang 3
Affiliations

Affiliations

  • 1 Department of Clinical Pharmacy, The First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang 310000, China.
  • 2 Department of Cardiology, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325035, China. Electronic address: 292854384@qq.com.
  • 3 The Third Affiliated Hospital of Zhejiang Chinese Medical University, Hangzhou, Zhejiang 310000, China. Electronic address: 492960408@qq.com.
Abstract

Acute lung injury (ALI), a common critical disease in clinical practice, has a mortality rate as high as 30-40 %, yet currently, no effective treatment methods are available. Research on ALI indicated that inhibition of overexpressed inflammatory factors might be a potential treatment for ALI. In this study, a series of cinnamic acid derivatives were obtained by introducing diverse aminothiazole fragments into the natural product cinnamic acid. Among these derivatives, compound 22 displayed excellent activity of inhibiting the release of IL-6 in J774A.1 cells. Moreover, it also ameliorated the LPS-induced ALI in mouse model by suppressing cytokine expression, reducing lung edema and macrophage infiltration. These findings indicated that compound 22 might provide a new lead structure for the development of drugs for ALI.

Keywords

Acute lung injury; Anti-inflammatory; Cinnamic acid derivatives.

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