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Total syntheses of lorneic acids F, H, and (±)-K and potential biological evaluation
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DOI：10.1016/j.rechem.2026.103281.png)
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Abstract
En 中文
We report the first total syntheses of lorneic acids F, H, and (+/-)-K, in 3 to 4 steps, from commercially available 2bromo-5-methylbenzaldehyde in 60%, 71%, and 59% overall yields, respectively. A key feature of the syntheses includes a Suzuki cross-coupling reaction to connect the carboxylic acid sidearms to the aromatic core in the natural products. Bioassays of lorneic acids A, C, D, F, H, J, and (+/-)-K identified their inhibition potency while molecular docking of these lorneic acids into the PDE5 active site provided insight into their possible interactions. The knowledge gained assisted us in identifying other lorneic acids and analogues that have the potential to exhibit enhanced PDE5 inhibition.
Keywords:
Actinomycetes
Lorneic acids F
H and (+/-)-K
PDE5 inhibitor
Suzuki cross-coupling reaction
Total synthesis
Molecular operating environment (MOE)
Docking
Ligand-binding interactions
Journal
IF:
4.2
Papers:
506
Citations:
6.1K
