Zobrazeno 1 - 3
of 3
pro vyhledávání: '"Yuichi Tokumaru"'
Autor:
Tetsuaki Hiyoshi, Dai Nozawa, Sora Kirinuki, Daiji Kambe, Yuichi Tokumaru, Ryo Suzuki, Mari Ohmichi, Hiroshi Kawamoto, Yunoshin Tamura, Futamura Aya, Takeshi Aoki, Noriko Hino
Publikováno v:
Bioorganicmedicinal chemistry. 28(13)
Here, we present the design, synthesis, and SAR of dual orexin 1 and 2 receptor antagonists, which were optimized by balancing the antagonistic activity for orexin receptors and lipophilicity. Based on the prototype compound 1, ring construction and
Autor:
Futamura Aya, Dai Nozawa, Seiken Tokura, Yuichi Tokumaru, Yuko Araki, Norikazu Ohtake, Yunoshin Tamura, Hiroshi Kawamoto, Sora Kakihara, Takeshi Aoki
Publikováno v:
Bioorganic & Medicinal Chemistry. 25:5203-5215
The design, synthesis, and structure activity relationships of the novel class of pyrazolylethylbenzamide orexin receptor 1-selective antagonists are described. Further derivatization of the prototype dual orexin receptor 1/2 antagonist lead (1) by i
0004 TS-142: A Novel and Potent Dual Orexin Receptor Antagonist with Sleep-Promoting Effects in Rats
Publikováno v:
Sleep. 43:A2-A2
Introduction The orexin system plays a pivotal role in regulating sleep and wakefulness, thus, orexin receptors (OX1 and OX2 receptors) have gained much attention as promising therapeutic targets for the treatment of insomnia. We synthesized a novel