1217441-35-4Relevant academic research and scientific papers
Discovery of potent and orally active tricyclic-based FBPase inhibitors
Tsukada, Tomoharu,Kanno, Osamu,Yamane, Takahiro,Tanaka, Jun,Yoshida, Taishi,Okuno, Akira,Shiiki, Takeshi,Takahashi, Mizuki,Nishi, Takahide
, p. 5346 - 5351 (2010)
With the aim of exploring the effect of tricyclic-based FBPase inhibitors in cells and in vivo, a series of prodrugs of tricyclic phosphonates was designed and synthesized. Introducing prodrug moieties into tricyclic-based phosphonates led to the discover
A prodrug approach towards the development of tricyclic-based FBPase inhibitors
Tsukada, Tomoharu,Tamaki, Kazuhiko,Tanaka, Jun,Takagi, Toshiyuki,Yoshida, Taishi,Okuno, Akira,Shiiki, Takeshi,Takahashi, Mizuki,Nishi, Takahide
scheme or table, p. 2938 - 2941 (2010/08/05)
For the purpose of reducing the strong CYP3A4 inhibitory potency of diamide prodrug 4, cyclic prodrugs of tricyclic-based FBPase inhibitors were synthesized. Extensive SAR studies led to the discovery of pyridine-containing cyclic prodrug 20, which strong
Structure-based drug design of tricyclic 8H-indeno[1,2-d][1,3]thiazoles as potent FBPase inhibitors
Tsukada, Tomoharu,Takahashi, Mizuki,Takemoto, Toshiyasu,Kanno, Osamu,Yamane, Takahiro,Kawamura, Sayako,Nishi, Takahide
scheme or table, p. 1004 - 1007 (2010/06/16)
With the goal of improving metabolic stability and further enhancing FBPase inhibitory activity, a series of tricyclic 8H-indeno[1,2-d][1,3]thiazoles was designed and synthesized with the aid of structure-based drug design. Extensive SAR studies led to th
