Combining Experimental Assays and Molecular Modeling to Evaluate Monosubstituted Cinnamic Acid Derivatives as PDE4B Inhibitors.

ABSTRACT: In this study, we evaluated the inhibitory effects of cinnamic acid and its 18 commercially available derivatives on phosphodiesterase 4 (PDE4) to investigate their therapeutic potential for chronic obstructive pulmonary disease (COPD). Among the tested compounds, p-coumaric acid and trans-4-methoxycinnamic acid exhibited potent PDE4B inhibitory activity (IC₅₀ = 2.2 μM and 8.2 μM, respectively) and notable selectivity over PDE4D, with IC₅₀ values against TNF-α release in human mononuclear cells of 21.5 μM and 30.8 μM, respectively, comparable to rolipram. Structure-activity relationship (SAR) analysis indicated that para-substituted derivatives generally showed higher activity than their meta- or ortho-substituted counterparts. A val

SUBMITTER: Zhao D 

PROVIDER: S-EPMC12750277 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature