1421335-97-8Relevant academic research and scientific papers
Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1
Udagawa, Shuji,Sakami, Satoshi,Takemura, Takahiro,Sato, Mikiya,Arai, Takahiro,Nitta, Aiko,Aoki, Takumi,Kawai, Koji,Iwamura, Tomokatsu,Okazaki, Seiji,Takahashi, Takehiro,Kaino, Mie
supporting information, p. 1617 - 1621 (2013/04/10)
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, which furthermore showed the potent efficacy in in vivo studies.
