Selective acetamidine-based nitric oxide synthase inhibitors: synthesis, docking, and biological studies

…, R Paciotti, A Ammazzalorso, B De Filippis…

文献索引：MacCallini, Cristina; Patruno, Antonia; Lannutti, Fabio; Ammazzalorso, Alessandra; De Filippis, Barbara; Fantacuzzi, Marialuigia; Franceschelli, Sara; Giampietro, Letizia; Masella, Simona; Felaco, Mario; Re, Nazzareno; Amoroso, Rosa Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6495 - 6499

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被引用次数: 5

摘要

N-[(3-Aminomethyl) benzyl] acetamidine derivatives were synthesized and in vitro evaluated as inhibitors of the inducible isoform of nitric oxide synthase (iNOS). Because of the high potency of action and the excellent selectivity over the endothelial nitric oxide synthase (eNOS), compound 10 was ex vivo evaluated on isolated and perfused resistance arteries. The results confirm that compound 10 selectively inhibits the iNOS, without affecting the ...