| Literature DB >> 14643355 |
Masaaki Hirose1, Shin-ichiro Egashira, Yasuhiro Goto, Takashi Hashihayata, Norikazu Ohtake, Hisashi Iwaasa, Mikiko Hata, Takehiro Fukami, Akio Kanatani, Koji Yamada.
Abstract
The identification of potent and selective orexin-2 receptor (OX(2)R) antagonists is described based on the modification of N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline analogue 1, recently discovered during high throughput screening (HTS). Substitution of an acyl group in 1 with tert-Leucine (tert-Leu), and introduction of a 4-pyridylmethyl substituent onto the amino function of tert-Leu improved compound potency, selectivity, and water solubility. Thus, compound 29 is a promising tool to investigate the role of orexin-2 receptors.Entities:
Mesh：
Substances：
Year: 2003 PMID： 14643355 DOI： 10.1016/j.bmcl.2003.08.038
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823