170376-11-1Relevant academic research and scientific papers
Synthesis of novel 1α,25-dihydroxy-19-norvitamin D3 with an amide conjugate
Suhara, Yoshitomo,Ono, Keiichiro,Yoshida, Akihiro,Fujishima, Toshie,Saito, Nozomi,Honzawa, Shinobu,Kishimoto, Seishi,Sugiura, Takayuki,Waku, Keizo,Takayama, Hiroaki,Kittaka, Atsushi
, p. 423 - 436 (2007/10/03)
The diene system of 1α,25-dihydroxy-19-norvitamin D3 was replaced by a stable amide bond. A 3-hydroxypropoxy group, which was effective on enhancing binding affinity of 1α,25-dihydroxyvitamin D3 for vitamin D receptor (VDR), was introduced to the C2-position of the amide type analogue of 1α,25-dihydroxy-19-norvitamin D3. The amide analogue was found to be not suitable for binding to the ligand binding domain of the bovine thymus VDR, and additional modification at the C2-position did not improve the affinity. Potency in induction of HL-60 cell differentiation was evaluated for the novel amide analogues (3a-c).
Fragmentation of carbohydrate anomeric alkoxy radicals. Synthesis of polyhydroxy piperidines and pyrrolidines related to carbohydrates
Francisco,Freire,Gonzalez,Leon,Riesco-Fagundo,Suarez
, p. 1861 - 1866 (2007/10/03)
Imino sugars of the piperidine and pyrrolidine types can be specifically obtained when protected 5-amino-5-deoxyfuranopentoses, 5-amino-5-deoxyfuranohexoses, 6-amino-6-deoxyfuranohexoses, and 6-amino-6-deoxypyranohexoses undergo a tandem alkoxy radical β-fragmentation-intramolecular cyclization reaction. The reaction is promoted by the system: iodosylbenzene - iodine under mild conditions. The tert-butoxycarbonyl, benzyloxycarbonyl, and diphenylphosphinoyl radicals have been studied as amino-protecting groups. Using this methodology, polyhydroxylated pyrrolidines of the D-erythrofuranoses 34 and 35, D-threofuranose 36, L-xylofuranose 42, and D-arabinofuranose 43 series and polyhydroxylated piperidines of the D-arabinopyranose type 37 and 38 were obtained.
1-N-Iminosugars: Potent and selective inhibitors of β-glycosidases
Ichikawa, Yoshitaka,Igarashi, Yasuhiro,Ichikawa, Mie,Suhara, Yoshitomo
, p. 3007 - 3018 (2007/10/03)
A series of 1-N-iminosugars were synthesized to supply the need for glycosidase inhibitors that are both highly potent and selective for β- glycosidases. Designed on the basis of the transition-state model of the β- glucosidase reaction, these iminosugar
An extremely potent inhibitor for β-galactosidase
Ichikawa, Yoshitaka,Igarashi, Yasuhiro
, p. 4585 - 4586 (2007/10/02)
A new galactose-type iminosugar in which a nitrogen atom is in the anomeric position was synthesized and was found to be an extremely potent inhibitor for β-galactosidase with Ki = 4 nM.
