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ID: ALA1136028
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. Part 1: synthesis and biological evaluation of dihydropyridin-2-imines.
Authors: Kawanaka Y, Kobayashi K, Kusuda S, Tatsumi T, Murota M, Nishiyama T, Hisaichi K, Fujii A, Hirai K, Naka M, Komeno M, Nakai H, Toda M.
Abstract: Dihydropyridin-2-imines were synthesized and biologically evaluated both in vitro and in vivo using a nitric oxide inhibition assay. Compounds 1, 4, 5 and 7-11 exhibited potent activity in the inducible nitric oxide (iNOS) inhibition assay. Of these 5, 6, 9 and 10 showed 5- to 11-fold increases in isoform selectivity. Compounds 1, 5, 9 and 10 showed potent inhibitory activity in the NOx accumulation assay in mice. Compounds 1 and 5 also showed good bioavailability (BA) when given orally.
CiteXplore: 12161118