Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1

…, K Kawai, T Iwamura, S Okazaki, T Takahashi…

文献索引：Udagawa, Shuji; Sakami, Satoshi; Takemura, Takahiro; Sato, Mikiya; Arai, Takahiro; Nitta, Aiko; Aoki, Takumi; Kawai, Koji; Iwamura, Tomokatsu; Okazaki, Seiji; Takahashi, Takehiro; Kaino, Mie Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1617 - 1621

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被引用次数: 3

摘要

A series of novel 5-trans-hydroxyadamantan-2-yl-5, 6, 7, 8-tetrahydropyrazolo [4, 3-c] azepin- 4 (1H)-ones that inhibit 11beta-hydroxysteroid dehydrogenase type 1 are described. We discovered these 7-membered cyclic amide derivatives by introducing a distinctive linker through pharmacophore analysis of known ligands included in X-ray co-crystal structures. Further optimization using docking studies led to highly potent inhibitors 15b and 27, ...