Design and synthesis of inhibitors of inducible nitric oxide synthase. Discovery of a new chemical lead with potential for oral bioavailability

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

Index: Kawanaka, Yasufumi; Kobayashi, Kaoru; Kusuda, Shinya; Tatsumi, Tadashi; Murota, Masayuki; Nishiyama, Toshihiko; Hisaichi, Katsuya; Fujii, Atsuko; Hirai, Keisuke; Naka, Masao; Komeno, Masaharu; Nakai, Hisao; Toda, Masaaki European Journal of Medicinal Chemistry, 2003 , vol. 38, # 3 p. 277 - 288

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Citation Number: 10

Abstract

A series of 2-iminopiperidines fused to small-membered rings (Tables 1 and 2) were synthesised and biologically evaluated using an in vitro human nitric oxide synthase (NOS) inhibition assay. Fused bicyclic compounds 5–9 exhibited nearly the same potency as compound 1 in the hiNOS inhibition assay. Among these, the 1-methyl analogues 8 and 9 showed better isoform selectivity than their corresponding unsubstituted analogues 7 and ...