1044239-14-6Relevant academic research and scientific papers
Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists
Sakamoto, Toshihiro,Moriya, Minoru,Haga, Yuji,Takahashi, Toshiyuki,Shibata, Takunobu,Okamoto, Osamu,Nonoshita, Katsumasa,Kitazawa, Hidefumi,Hidaka, Masayasu,Gomori, Akira,Iwaasa, Hisashi,Ishihara, Akane,Kanatani, Akio,Fukami, Takehiro,Gao, Ying-Duo,MacNeil, Douglas J.,Yang, Lihu
scheme or table, p. 1564 - 1568 (2009/12/07)
A series of spiroindoline-3,4′-piperidine derivatives were synthesized and evaluated for their binding affinities and antagonistic activities at Y5 receptors. Potent Y5 antagonists were tested for their oral bioavailabilities and brain penetration in rats
Novel orally active NPY Y5 receptor antagonists: Synthesis and structure-activity relationship of spiroindoline class compounds
Sakamoto, Toshihiro,Moriya, Minoru,Tsuge, Hiroyasu,Takahashi, Toshiyuki,Haga, Yuji,Nonoshita, Katsumasa,Okamoto, Osamu,Takahashi, Hirobumi,Sakuraba, Aya,Hirohashi, Tomoko,Shibata, Takunobu,Kanno, Tetsuya,Ito, Junko,Iwaasa, Hisashi,Gomori, Akira,Ishihara, Akane,Fukuroda, Takahiro,Kanatani, Akio,Fukami, Takehiro
experimental part, p. 5015 - 5026 (2009/12/04)
Spiroindoline urea derivatives, designed to act as NPY Y5 receptor antagonists, were synthesized and their structure-activity relationships were investigated. Of these derivatives, compound 3a showed good Y5 binding affinity with favorable pharmacokinetic
False positives in a reporter gene assay: Identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase
Heitman, Laura H.,Van Veldhoven, Jacobus P. D.,Zweemer, Annelien M.,Ye, Kai,Brussee, Johannes,Ijzerrnan, Adriaan P.
supporting information; experimental part, p. 4724 - 4729 (2009/06/18)
Luciferase reporter-gene assays are a commonly used technique in high-throughput screening campaigns. In this study, we report on a luciferase inhibitor (1), which emerged from an antagonistic G protein-coupled receptor luciferase reporter-gene assay scre
