Synthesis and Biological Evaluation of α-L-Fucosidase Inhibitors: 5a-Carba-α-L-fucopyranosylamine and Related Compounds

Autor: Takashi Odagiri, Hironobu Hashimoto, Hideya Yuasa, Ayako Maruyama, Seiichiro Ogawa
Rok vydání: 2001
Předmět:
Zdroj: European Journal of Organic Chemistry. 2001:967-974
ISSN: 1099-0690
1434-193X
DOI: 10.1002/1099-0690(200103)2001:5<967::aid-ejoc967>3.0.co;2-j
Popis: 5a-Carba-α-L-fucopyranosylamine (5), an α-glucosidase inhibitor validamine analog possessing an α-L-fucose-type structure, and four related compounds (4 and 6−8) were synthesized and their glycosidase inhibitory potential determined. Carbafucosylamine has already been shown to possess a specific and very strong inhibitory activity against α-L-fucosidase (Ki = 1.2 × 10−8M, bovine kidney). Judging from the activity of the other analogs prepared, this amine might be expected to be a lead compound for development of a new type of α-L-fucosidase inhibitor.
Databáze: OpenAIRE