- Visible-Light-Driven C?H Oxidation of Cyclic Tertiary Amines: Access to Synthetic Strychnos Alkaloids with Antiviral Activity
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Air and visible light have been used in facile direct C?H oxidation of cyclic tertiary amines at ambient conditions, employing organic dyes as photocatalysts and LED. Tolerance of this new environmentally compatible protocol to various side-chain derivati
- Guryev, Anton A.,Hahn, Friedrich,Marschall, Manfred,Tsogoeva, Svetlana B.
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supporting information
p. 4062 - 4066
(2019/03/07)
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- Design, synthesis, and biological evaluation of novel (1-thioxo-1,2,3,4- tetrahydro-β-carbolin-9-yl)acetic acids as selective inhibitors for AKR1B1
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New substituted (1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acids were designed as the inhibitor of AKR1B1 based upon the structure of rhetsinine, a minor alkaloidal component of Evodia rutaecarpa, and twenty derivatives were synthesized and evaluated. The most active compound of the series was (2-benzyl-6-methoxy-1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl) acetic acid (7m), which showed comparable inhibitory activity for AKR1B1 (IC50 = 0.15 μM) with clinically used epalrestat (IC50 = 0.1 μM). In the view of activity and selectivity, the most potent compound was (2-benzyl-6-carboxy-1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acid (7t), which showed strong inhibitory effect (IC50 = 0.17 μM) and very high selectivity for AKR1B1 against AKR1A1 (311:1) and AKR1B10 (253:1) compared with epalrestat.
- Minehira, Daisuke,Takeda, Daisuke,Urata, Hirokazu,Kato, Atsushi,Adachi, Isao,Wang, Xu,Matsuya, Yuji,Sugimoto, Kenji,Takemura, Mayuko,Endo, Satoshi,Matsunaga, Toshiyuki,Hara, Akira,Koseki, Jun,Narukawa, Kayo,Hirono, Shuichi,Toyooka, Naoki
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scheme or table
p. 356 - 367
(2012/03/09)
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- REACTION OF ARYLHYDRAZINES WITH α-FORMYLBUTYROLACTAM DERIVATIVES
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The Vilsmeier formylation of butyrolactam and N-phenylbutyrolactam has given their α-dimethylaminomethylene derivatives.The reaction of the latter with α-substituted arylhydrazines leads to the formation of 1-oxo-1,2,3,4-tetrahydro-β-carbolines.When unsub
- Tokmakov, G. P.,Zemyanova. T. G.,Grandberg, I. I.
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