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Design, Synthesis, and Anti-Inflammation Activity of C-12 Arylated Tetrahydropalmatine Derivatives
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DOI：10.1002/cmdc.70355.png)
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Abstract
En 中文
Structural optimization of natural products provides an important way for new drug discovery. The bioactive natural product L-tetrahydropalmatine and its analogs have attracted significant attention due to their potent pharmacological activities. In this study, a library of novel C12-arylated L-tetrahydropalmatine derivatives (4a–4ad) was synthesized via Pd-catalyzed Suzuki–Miyaura cross-coupling reaction. Among these derivatives, compound 4p, bearing a 4-ethenylphenyl moiety, suppressed the production of pro-inflammatory cytokines (TNF-α and IL-1β) in LPS-induced in vitro inflammatory models, indicating that it might be a potential anti-inflammatory agent. This work offers valuable insights into the development of tetrahydropalmatine analogs as novel anti-inflammatory agents.
Keywords:
anti-inflammation activity
pro-inflammatory cytokines
Suzuki–Miyaura cross-coupling
tetrahydropalmatine
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