Discovery of orexin 2 receptor selective and dual orexin receptor agonists based on the tetralin structure: Switching of receptor selectivity by chirality on the tetralin ring

Autor:	Keita Iio, Tsuyoshi Saitoh, Ryuichiro Ohshita, Tsubasa Hino, Mao Amezawa, Yoshiaki Takayama, Yasuyuki Nagumo, Naoshi Yamamoto, Noriki Kutsumura, Yoko Irukayama-Tomobe, Yukiko Ishikawa, Ryuji Tanimura, Masashi Yanagisawa, Hiroshi Nagase
Rok vydání:	2021
Předmět:	Structure-Activity Relationship Dose-Response Relationship Drug Molecular Structure Tetrahydronaphthalenes Orexin Receptors Organic Chemistry Clinical Biochemistry Drug Discovery Pharmaceutical Science Molecular Medicine Humans Molecular Biology Biochemistry
Zdroj:	Bioorganicmedicinal chemistry letters. 60
ISSN:	1464-3405
Popis:	A novel series of 1-amino-tetralin derivatives were designed and synthesized based on the putative binding mode of the naphthalene-type orexin receptor agonist 5 and their agonist activities against orexin receptors were evaluated. The introduction of N-methyl-(3-methoxyphenyl)acetamide unit onto the 1-amino-tetralin skeleton remarkably enhanced the potency of the agonist. The asymmetric synthesis of 6 revealed that (-)-6 having a (S)-1-amino-tetralin skeleton showed a OX
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8aae6454ae5d938fb321fbcadcbfd765 https://pubmed.ncbi.nlm.nih.gov/35051577 Zobrazit plný text záznamu Full Text from ScienceDirect