1414960-66-9Relevant academic research and scientific papers
1-((1H-PYRAZOL-4-YL)METHYL)-3-(PHENYL)-1,3-DIHYDRO-2H-IMIDAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS GPR139 ANTAGONISTS FOR THE TREATMENT OF E.G. DEPRESSION
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Paragraph 000416-000417, (2021/11/26)
The present invention refers to compounds of formula (I). The present invention also relates to compounds of formula (I) for use as G Protein coupled Receptor 139 (GPR139) antagonists in methods of medical treatment of e.g. depression, Alzheimer's disease
A Unified Strategy for the Synthesis of β-Carbolines, γ-Carbolines, and Other Fused Azaheteroaromatics under Mild, Metal-Free Conditions
Uredi, Dilipkumar,Motati, Damoder Reddy,Blake Watkins
supporting information, p. 6336 - 6339 (2018/10/15)
An efficient, unified approach for the synthesis of β-carbolines, γ-carbolines, and other fused azaheteroaromatics has been realized under metal-free conditions, from propargylic amines and (hetero)aromatic aldehydes. This unified strategy provides β- and
1,5-Disubstituted 1,2,3-Triazole-Containing Peptidotriazolamers: Design Principles for a Class of Versatile Peptidomimetics
Kracker, Oliver,Góra, Jerzy,Krzciuk-Gula, Joanna,Marion, Antoine,Neumann, Beate,Stammler, Hans-Georg,Nie?, Anke,Antes, Iris,Latajka, Rafa?,Sewald, Norbert
supporting information, p. 953 - 961 (2017/12/26)
Peptidotriazolamers are hybrid foldamers combining features of peptides and triazolamers—repetitive peptidomimetic structures with triazoles replacing peptide bonds. We report on the synthesis of a new class of peptidomimetics, containing 1,5-disubstituted 1,2,3-triazoles in an alternating fashion with amide bonds and the analysis of their conformation in solid state and solution. Homo- or heterochiral peptidotriazolamers were obtained from enantiomerically pure propargylamines with stereogenic centers in the propargylic position and α-azido esters by ruthenium-catalyzed azide–alkyne cycloaddition (RuAAC) under microwave conditions in high yields. With such building blocks the peptidotriazolamers are readily available by solution phase synthesis. While the conformation of the homochiral peptidotriazolamer Boc-Ala[5Tz]Phe-Val[5Tz]Ala-Leu[5Tz]Val-OBzl resembles that of a β VIa1 turn, the heterochiral peptidotriazolamer Boc-d-Ala[5Tz]Phe-d-Val[5Tz]Ala-d-Leu[5Tz]Val-OBzl adopts a polyproline-like repetitive structure.
Cascade electrophilic iodocyclization: Efficient preparation of 4-iodomethyl substituted tetrahydro-β-carbolines and formal synthesis of oxopropaline G
Song, Hongjian,Liu, Yongxian,Wang, Qingmin
supporting information, p. 3274 - 3277 (2013/07/26)
4-Iodomethyl substituted tetrahydro-β-carbolines, the core structure of numerous natural products and bioactive molecules, are readily prepared via I2-promoted cascade electrophilic cyclization. The reactivity differences of olefins and alkynes
Synthesis and bioactivities of novel N-(4-(2-Aryloxythiazol-5-yl)but-3-yn- 2-yl)benzamides
Zhu, Youquan,Liu, Pei,Wang, Danyang,Zhang, Jin,Cheng, Jie,Ma, Yuan,Zou, Xiaomao,Yang, Huazheng
, p. 173 - 181 (2013/08/24)
A series of novel N-(4-(2-aryloxythiazol-5-yl)but-3-yn-2-yl)benzamide derivatives were designed and synthesized. Their structures were identified by 1H NMR and elemental analyses. Preliminary bioassays indicated that some title compounds provided >80% control of Sclerotinia sclerotiorum at 50 μg/mL and >70% herbicidal activities against B. campestris at 100 μg/mL. Their structure-activities relationships were also discussed. A series of novel N-(4-(2-aryloxythiazol-5-yl)but-3-yn-2-yl)benzamide derivatives were designed and synthesized. Some of them provided >80% control of Sclerotinia sclerotiorum at 50 μg/mL and >70% herbicidal activities against B. campestris at 100 μg/mL. Copyright
Psychoactive propargylamine derivatives used in the treatment of anxiety, psychotic states or aggression
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, (2008/06/13)
Propargylamine derivatives having the general formula: STR1 wherein R is a hydrogen atom, an unsubstituted phenyl group or a phenyl group substituted with halogen, trifluoromethyl, loweralkoxy, nitro, cyano, amido or N,N-diloweralkylamido, R1,
