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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Murata, T. et al.

Murata, Shimada, Sakakibara, Yoshino, Masuda, Shintani, Sato, Koriyama, Fukushima, Nunami, Yamauchi, Fuchikami, Komura, Watanabe, Ziegelbauer, Bacon, Lowinger,

Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents.

A series of 2-amino-3-cyano-4-alkyl-6-(2-hydroxyphenyl)pyridine derivatives was synthesized and evaluated as I kappaB kinase beta ( IKK-beta) inhibitors. Modification of a novel IKK-beta inhibitor 1 ( IKK-beta IC(50)=1500 nM, Cell IC(50)=8000 nM) at the 4-phenyl ring and 6-phenol group on the pyridine core ring resulted in a marked increased in biological activities. An optimized compound, 2-amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-piperidin-4-yl nicotinonitrile, exhibited excellent in vitro profiles ( IKK-beta IC(50)=8.5 nM, Cell IC(50)=60 nM) and a strong oral efficacy in in vivo anti-inflammatory assays (significant effects at 1mg/kg, po in arachidonic acid-induced ear edema model in mice).[1]

References

Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents. Murata, T., Shimada, M., Sakakibara, S., Yoshino, T., Masuda, T., Shintani, T., Sato, H., Koriyama, Y., Fukushima, K., Nunami, N., Yamauchi, M., Fuchikami, K., Komura, H., Watanabe, A., Ziegelbauer, K.B., Bacon, K.B., Lowinger, T.B. Bioorg. Med. Chem. Lett. (2004) [Pubmed]

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