Synthesis of imifuramine and its stereoisomers exhibiting histamine H3-agonistic activity
β Scribed by Shinya Harusawa; Tomonari Imazu; Seiichiroh Takashima; Lisa Araki; Hirofumi Ohishi; Takushi Kurihara; Yumiko Yamamoto; Atsushi Yamatodani
- Publisher
- Elsevier Science
- Year
- 1999
- Tongue
- French
- Weight
- 248 KB
- Volume
- 40
- Category
- Article
- ISSN
- 0040-4039
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β¦ Synopsis
The four possible stereoisomers of a novel imidazole C-nucleoside derivative were synthesized by the eJJ~cient use of a PhSe group. Among them, ( + )-4( 5)-[(2R,5R)-5-(aminomethyl)tetrahydrofuran-2-yl]imidazole (imifuramine) was indicated as a novel type of histamine Hj-agon/st by a brain microdialysis method.
π SIMILAR VOLUMES
## Abstract It is shown that the quality of action of the synthesized compounds, their potency and receptor subtype selectivity depend on the stereochemistry.
N Ξ± -Alkylated Derivatives of 2-Phenylhistamines: Synthesis and in vitro Activity of Potent Histamine H 1 -Receptor Agonists. -In vitro study of new potent histamine H 1 -receptor agonists, e.g. (V), shows that the derivative (Va) is the most potent compound described in the literature until now. -