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• W1983175066 abstract "Toll-like receptor 4 (TLR4), a membrane spanning receptor protein that functions in complex with its accessory protein MD-2, is an intriguing target for therapeutic development. Herein we report the identification of a series of novel TLR4 inhibitors and the development of a robust, enantioselective synthesis using an unprecedented Mannich-type reaction to functionalize a pyrazole ring. In silico and cellular assay results demonstrated that compound 1 and its analogues selectively block TLR4 activation in live cells. Animal model tests showed that 1 and its derivatives could potentiate morphine-induced analgesia in vivo, presumably by attenuating the opioid-induced TLR4 activation." @default.
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• W1983175066 date "2010-05-14" @default.
• W1983175066 modified "2023-10-14" @default.
• W1983175066 title "Selection, Preparation, and Evaluation of Small-Molecule Inhibitors of Toll-Like Receptor 4" @default.
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• W1983175066 doi "https://doi.org/10.1021/ml100041f" @default.
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