Identification of N-benzyltetrahydroisoquinolines as novel anti-neuroinflammatory agents

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2018-11
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English
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Abstract

A series of simplified berberine analogs was designed, synthesized, and evaluated for anti-inflammatory activity. SAR studies identified N-benzyltetrahydroisoquinoline 7d as a potent berberine analog. 7d suppressed LPS-induced inflammatory cytokine levels in both BV2 cells and primary microglia. Taken together, our results suggest that simplified BB analogs have therapeutic potential as a novel class of anti-neuroinflammatory agents.

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Gabet, B., Kuo, P.-C., Fuentes, S., Patel, Y., Adow, A., Alsakka, M., … Brown, D. A. (2018). Identification of N-benzyltetrahydroisoquinolines as novel anti-neuroinflammatory agents. Bioorganic & Medicinal Chemistry. https://doi.org/10.1016/j.bmc.2018.10.020
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Bioorganic & Medicinal Chemistry
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