Synthesis of phenylalkyl-substituted polyhydroxypiperidines as potent inhibitors for α-l-fucosidase

Saka T.; Okaki T.; Ifuku S.; Yamashita Y.; Sato K.; Miyawaki S.; Kamori A.; Kato A.; Adachi I.; Tezuka Y.; Kiria P.G.; Onomura O.; Minato D.; Sugimoto K.; Matsuya Y.; Toyooka N.

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Synthesis of phenylalkyl-substituted polyhydroxypiperidines as potent inhibitors for α-l-fucosidase

机译：苯烷基取代的多羟基哌啶类化合物作为α-1-岩藻糖苷酶有效抑制剂的合成

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Synthesis and inhibitory activities against α-l-fucosidase of phenylalkyl-substituted polyhydroxypiperidines have been described. Among the newly synthesized compounds, 2,4,6-trichloro derivative (16q) showed very high inhibitory activity against α-l-fucosidase with IC50 value of 0.005 μM, and Ki values of 0.0011 μM, respectively.

机译：已经描述了苯烷基取代的多羟基哌啶的合成及其对α-1-岩藻糖苷酶的抑制活性。在新合成的化合物中，2,4,6-三氯衍生物（16q）对α-1-岩藻糖苷酶的抑制活性非常高，IC50值为0.005μM，Ki值为0.0011μM。

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《Tetrahedron》 |2013年第49期|共9页
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Saka T.; Okaki T.; Ifuku S.; Yamashita Y.; Sato K.; Miyawaki S.; Kamori A.; Kato A.; Adachi I.; Tezuka Y.; Kiria P.G.; Onomura O.; Minato D.; Sugimoto K.; Matsuya Y.; Toyooka N.;
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正文语种 eng
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关键词
α-l-fucosidase; C-1 phenylalkyl-substituted polyhydroxypiperidine; Iminosugar; l-Fucose;

机译：α-1-岩藻糖苷酶;C-1苯基烷基取代的多羟基哌啶;亚氨基糖;1-岩藻糖;

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1. Synthesis of phenylalkyl-substituted polyhydroxypiperidines as potent inhibitors for α-l-fucosidase [J] . Saka T., Okaki T., Ifuku S., Tetrahedron . 2013,第49期

机译：苯烷基取代的多羟基哌啶类化合物作为α-1-岩藻糖苷酶有效抑制剂的合成
2. gem-diamine 1-N-iminosugars of L-fucose-type, the extremely potent L-fucosidase inhibitors. [J] . Shitara E, Nishimura Y, Kojima F, Bioorganic and medicinal chemistry . 2000,第2期

机译：L-岩藻糖型的宝石二胺1-N-亚氨基糖，一种非常有效的L-岩藻糖苷酶抑制剂。
3. Looking glass inhibitors: synthesis of a potent naringinase inhibitor L-DIM [1,4-dideoxy-1,4-imino-L-mannitol], the enantiomer of DIM [1,4-dideoxy-1,4-imino-D-mannitol] a potent alpha-D-mannosidase inhibitor [J] . Hakansson AE, van Ameijde J, Gughelmini L, Tetrahedron, Asymmetry: The International Journal for Repid Publication on all Aspects of Asymmetry in Orgainc, Inorganic, Organometallic, Physical and Bio-Organic Chemistry . 2007,第2期

机译：窥镜抑制剂：合成有效的柚皮苷酶抑制剂L-DIM [1,4-dideoxy-1,4-imino-L-甘露醇]，DIM的对映异构体[1,4-dideoxy-1,4-imino-D-甘露醇]一种有效的α-D-甘露糖苷酶抑制剂
4. Design, Synthesis, and Cytoprotective Effect of 2-Aminothiazole Analogues as Potent Poly(ADP-Ribose) Polymerase-1 Inhibitors [C] . Wen-Ting Zhang, Gang-Ying Chen, Yi-Jing Zhu, ICMSI;International conference of molecular simulations and applied informatics technologies . 2010

机译：2-氨基噻唑类似物作为强力聚（ADP-核糖）聚合酶-1抑制剂的设计，合成和细胞保护作用
5. Synthesis and Utility of New Ynamide and Organo-allyltrifluoroborate Reagents: Application to the Total Synthesis of Geralcin A, Hydrazidomycins A-B, (±)-CPC–1, (±)-Alline, Splenocin-B, and the Potent Cancer Cell Growth Inhibitors Kitastatin and Respirantin [D] . Beveridge, Ramsay Eaton 2014

机译：新型酰胺和有机烯丙基三氟硼酸盐试剂的合成与应用：在Geralcin A，Hydrazidomycins AB，（±）-CPC-1，（±）-Alline，Splenocin-B和有效的癌细胞生长抑制剂Kitastatin的总合成中的应用和呼吸素
6. Synthesis of 2RS4RS-1-2-Phenyl-4-2-(2-trifluromethoxy-phenoxy)-ethyl-13-dioxolan-2-yl-methyl-1H-124-triazole Derivatives as Potent Inhibitors of Brassinosteroid Biosynthesis [O] . Kazuhiro Yamada, Yuko Yoshizawa, Keimei Oh 2012

机译：2RS4RS-1- 2-苯基-4- 2-（2-三氟甲氧基-苯氧基）-乙基 -13-二氧戊环-2-基-甲基 -1H-124-的合成三唑衍生物作为油菜素类固醇生物合成的有效抑制剂
7. A multidisciplinary study of 3-(β- d -glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors [O] . Sándor Kun, Jaida Begum, Efthimios Kyriakis, 2018

机译：3-（β-D-葡糖基）-5-取代的-1,2,4-三唑衍生物作为糖原磷酸化酶抑制剂的多学科研究：计算，合成，晶体学和动力学显示出新的有效抑制剂

Synthesis of phenylalkyl-substituted polyhydroxypiperidines as potent inhibitors for α-l-fucosidase

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