Synthesis and activity of 1-N-iminosugar inhibitors, siastatin B analogues for alpha-N-acetylgalactosaminidase and beta-N-acetylglucosaminidase.
N-Acetylgalactosamine-based 1-N-iminosugars, new types of glycosidase inhibitor have been synthesized by modeling on siastatin B, isolated from a Streptomyces culture. The analogues of siastatin B were proved to be potent inhibitors for alpha-N-acetylgalactosaminidase and/or beta-N-acetylglucosaminidase.
Nishimura
Y
Y
Institute of Microbial Chemistry, Tokyo, Japan.
Satoh
T
T
Kudo
T
T
Kondo
S
S
Takeuchi
T
T
D000118:Acetylglucosaminidase / Q000037:antagonists & inhibitors*; D000818:Animals; D002417:Cattle; D002645:Chickens; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004822:Epididymis / Q000187:drug effects / Q000201:enzymology; D006596:Hexosaminidases / Q000037:antagonists & inhibitors*; D050112:Imino Pyranoses; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D008297:Male; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D048809:alpha-N-Acetylgalactosaminidase
C100559:2-acetamido-5-hydroxymethylpiperidine-3,4-diol; D004791:Enzyme Inhibitors; D050112:Imino Pyranoses; D010880:Piperidines; C011353:siastatin; D006596:Hexosaminidases; D048809:alpha-N-Acetylgalactosaminidase; D000118:Acetylglucosaminidase