Ortho-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors

…, R de Jesus, A Yuan, RD Ghai, A Trapani…

文献索引：Ksander, Gary M.; De Jesus, Reynalda; Yuan, Andrew; Ghai; Trapani; McMartin, Colin; Bohacek, Regine Journal of Medicinal Chemistry, 1997 , vol. 40, # 4 p. 495 - 505

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被引用次数: 52

摘要

The design and preparation of ortho-substituted benzofused macrocyclic lactams are described. The benzofused macrocyclic lactams were designed as neutral endopeptidase 24.11 (NEP) inhibitors. Docking studies were carried out in a model of thermolysin (TLN) using the MACROMODEL and QXP modeling programs to select suitable ring sizes. These studies predicted that the 11-, 12-, and 13-membered ring macrocyclic lactams would be ...