Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. synthesis and biological evaluation of dihydropyridin-2 (1H)-imines and 1, 5, 6, …

Y Kawanaka, K Kobayashi, S Kusuda, T Tatsumi…

文献索引：Kawanaka, Yasufumi; Kobayashi, Kaoru; Kusuda, Shinya; Tatsumi, Tadashi; Murota, Masayuki; Nishiyama, Toshihiko; Hisaichi, Katsuya; Fujii, Atsuko; Hirai, Keisuke; Nishizaki, Minoru; Naka, Masao; Komeno, Masaharu; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 5 p. 689 - 702

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被引用次数: 15

摘要

The process of discovery and biological evaluation of α, β-unsaturated cyclic amidines, as selective inhibitors of inducible nitric oxide synthase (iNOS), is reported. Dihydropyridin-2 (1H)-imines and 1, 5, 6, 7-tetrahydro-2H-azepin-2-imines were synthesized and biologically evaluated both in vitro and in vivo using a nitric oxide synthase inhibition assay. Compounds 1, 5, 6, 8–12 and 16 exhibited potent inhibition of iNOS. Among these, compounds 6, 7, 10 ...