Design and synthesis of rho kinase inhibitors (III)

…, Y Tagami, M Sato, T Sugiyama, K Fukushima…

文献索引：Iwakubo, Masayuki; Takami, Atsuya; Okada, Yuji; Kawata, Takehisa; Tagami, Yoshimichi; Sato, Motoko; Sugiyama, Terumi; Fukushima, Kayoko; Taya, Shinichiro; Amano, Mutsuki; Kaibuchi, Kozo; Iijima, Hiroshi Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 2 p. 1022 - 1033

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被引用次数: 52

摘要

The structure–activity relationship of Rho kinase inhibitors bearing an isoquinoline scaffold was studied. N-(1-Benzyl-3-pyrrolidyl)-N-(5-isoquinolyl) amine analogues were optimized with respect to their inhibitory potencies for the enzyme and for chemotaxis. The potent analogues were further evaluated by an ex vivo test in which the selected compounds were orally administered to rats, and the Rho kinase inhibitory potency observed in the rat ...