Author/Authors :
Yasufumi Kawanaka، نويسنده , , Kaoru Kobayashi، نويسنده , , Shinya Kusuda، نويسنده , , Tadashi Tatsumi، نويسنده , , Masanori Murota، نويسنده , , Toshihiko Nishiyama، نويسنده , , Katsuya Hisaichi، نويسنده , , Atsuko Fujii، نويسنده , , Keisuke Hirai، نويسنده , , Masao Naka، نويسنده , , Masaharu Komeno، نويسنده , , Hisao Nakai، نويسنده , , Masaaki Toda، نويسنده ,
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.
