350-78-7Relevant academic research and scientific papers
A NOVEL PROCESS FOR THE PREPARATION OF TRYPTAMINES AND DERIVATIVES THEREOF
-
Page/Page column 18, (2017/05/10)
The present invention relates to a novel process for the preparation of tryptamine, its substituted derivatives and intermediates for the preparation of them.
METHOD FOR PRODUCING 4-FLUOROISATIN DERIVATIVE
-
Paragraph 0110, (2017/02/09)
PROBLEM TO BE SOLVED: To provide a method for producing a 4-fluoroisatin derivative including 4-fluoroisatin at high purity and at high yield. SOLUTION: Provided is a method for producing a 4-fluoroisatin, in a production process of a 4-fluoroisatin derivative represented by general formula (1), comprising: a step (A) where a toluene derivative represented by the general formula (2) is used as starting raw material, the toluene derivative is carbon-increased using DMFdialkylacetal, and thereafter, reduction is performed using a reducing agent and acid to synthesize an indol derivative represented by general formula (3); and a step (B) where the indol derivative is oxidized. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
Structure-based design, synthesis, andanticonvulsant activity of isatin-1-N-phenylacetamide derivatives
Xie, Chao,Tang, Li-Ming,Li, Fu-Nan,Guan, Li-Ping,Pan, Cheng-Yan,Wang, Si-Hong
, p. 2161 - 2168 (2014/05/06)
In an effort to develop the potent anticonvulsant agents, a series of novel isatin-1-N-phenylacetamide derivatives was synthesized and screened for their in vivo anticonvulsant activity against maximal electroshock test and evaluated for their neurotoxicity by the rotarod test at the same dose levels. Ten compounds exhibited the anticonvulsant activity. 2-(5-Methyl-2,3-dioxoindolin-1- yl)-N-phenylacetamide (4b) was found to be the most potent compound of the series with an ED50 of 91.3 mg/kg, TD50 of >1,000 mg/kg, a higher protective index (PI = TD50/ED50, >11) was gained than the reference drug phenobarbital and carbamazepine. The essential structural features responsible for interaction with receptor site are established within a suggested pharmacophore. Springer Science+Business Media 2013.
NITROGENATED HETEROCYCLIC COMPOUND AND AGRICULTURAL OR HORTICULTURAL FUNGICIDE
-
Paragraph 0379; 0380, (2014/03/25)
An agricultural or horticultural fungicide contains as an active ingredient thereof at least one compound selected from the group consisting of nitrogenated heterocyclic compounds represented by formula (I) (wherein, R represents a group represented by CR
Novel synthesis of 4-or 6-substituted indirubin derivatives
Zhang, Aiying,Yu, Mingfeng,Lan, Tian,Liu, Zenglu,Mao, Zhenmin
experimental part, p. 3125 - 3134 (2010/12/24)
A simple and convenient route for synthesis of a series of 4-or 6-substituted indirubin derivatives by oxidation and subsequent condensation of indoxyl and isatin is described. Acidic reaction conditions are crucial to the condensation of 4-substituted derivatives, whereas for the condensation of 6-substituted derivatives, both acidic and basic conditions work well. Copyright Taylor & Francis Group, LLC.
Counter-current chromatography separation of isatin derivatives using the sandmeyer methodology
Almeida, Ma?rcia R.,Leita?o, Gilda G.,Silva, Ba?rbara V.,Barbosa, Jussara P.,Pintoa, Angelo C.
scheme or table, p. 764 - 769 (2010/08/13)
A rapid and efficient method, using high-speed counter-current chromatography (HSCCC) technique, was developed for the separation of isomeric isatin derivatives, prepared following the Sandmeyer route. The biphasic solvent system composed of hexane:ethyl acetate:ethanol:water 1:0.5:0.5:1 (v/v/v/v) was used for all separations.
INDIRUBIN-TYPE COMPOUNDS, COMPOSITIONS, AND METHODS FOR THEIR USE
-
Page/Page column 23-24; Figure 2A, (2008/06/13)
Compounds and compositions including 6-bromo-indirubin, 5-amino-indirubin and N-methyl-indirubins and related indirubin derivatives are provided that are useful as selective modulators of glycogen synthase kinase-3, cyclin-dependent protein kinases or aryl hydrocarbon receptors. Methods of inhibiting or modulating cell growth or cell cycling are provided using the compounds of the invention. In other aspects, compounds and methods for the treatment of protozoan-mediated diseases, Alzheimer's disease and diabetes are provided.
Structural Basis for the Synthesis of Indirubins as Potent and Selective Inhibitors of Glycogen Synthase Kinase-3 and Cyclin-Dependent Kinases
Polychronopoulos, Panagiotis,Magiatis, Prokopios,Skaltsounis, Alexios-Leandros,Myrianthopoulos, Vassilios,Mikros, Emmanuel,Tarricone, Aldo,Musacchio, Andrea,Roe, S. Mark,Pearl, Laurence,Leost, Maryse,Greengard, Paul,Meijer, Laurent
, p. 935 - 946 (2007/10/03)
Pharmacological inhibitors of glycogen synthase kinase-3 (GSK-3) and cyclin-dependent kinases have a promising potential for applications against several neurodegenerative diseases such as Alzheimer's disease. Indirubins, a family of bis-indoles isolated from various natural sources, are potent inhibitors of several kinases, including GSK-3. Using the cocrystal structures of various indirubins with GSK-3β, CDK2 and CDK5/p25, we have modeled the binding of indirubins within the ATP-binding pocket of these kinases. This modeling approach provided some insight into the molecular basis of indirubins' action and selectivity and allowed us to forecast some improvements of this family of bis-indoles as kinase inhibitors. Predicted molecules, including 6-substituted and 5,6-disubstituted indirubins, were synthesized and evaluated as CDK and GSK-3 inhibitors. Control, kinase-inactive indirubins were obtained by introduction of a methyl substitution on N1.
