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Novel indole-based indoleamine 2,3-dioxygenase-1 (IDO1) inhibitors: design, synthesis, and antidepressant evaluation
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PRE
AI
J
W
Y
J
N
W
S
朱
M
J
甯
江
DOI：10.1016/j.bmc.2025.118503.png)
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Abstract
En 中文
• Scaffold hopping of known benzimidazole IDO1 inhibitors yielded novel potent indole-based leads. • Indole derivatives 9f and 10f achieve sub-10 nM IDO1 inhibition in cell-based bioassay. • Compound 10f suppresses neuroinflammation in LPS-stimulated BV-2 microglia. • Compounds 9f and 10f show improved plasma stability and extended in vivo half-life. • Both compounds rescue depressive-like behavior in LPS-induced mouse models.
Journal
B
IF:
3
Papers:
1.7W
Citations:
2.7W
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Cited Papers