29946-61-0Relevant academic research and scientific papers
Synthesis of zanthoxylamide protoalkaloids and their in silico ADME-Tox screening and in vivo toxicity assessment in zebrafish embryos
Puerto Galvis, Carlos E.,Kouznetsov, Vladimir V.
, p. 291 - 299 (2018/11/24)
Inspired by the simple and attractive structure of zanthoxylamide protoalkaloids: armatamide, rubecenamide, lemairamin, rubemamine and zanthosine; isolated from plants of the genus Zanthoxylum. We report the synthesis of a series of 29 substituted N-pheny
Dopaminergic isoquinolines with hexahydrocyclopenta[ ij ]-isoquinolines as D2-like selective ligands
Párraga, Javier,Andujar, Sebastián A.,Rojas, Sebastián,Gutierrez, Lucas J.,El Aouad, Noureddine,Sanz, M. Jesús,Enriz, Ricardo D.,Cabedo, Nuria,Cortes, Diego
, p. 27 - 42 (2016/07/06)
Dopamine receptors (DR) ligands are potential drug candidates for treating neurological disorders including schizophrenia or Parkinson's disease. Three series of isoquinolines: (E)-1-styryl-1,2,3,4-tetrahydroisoquinolines (series 1), 7-phenyl-1,2,3,7,8,8a
Design, synthesis, and evaluation of caffeic acid amides as synergists to sensitize fluconazole-resistant Candida albicans to fluconazole
Dai, Li,Zang, Chengxu,Tian, Shujuan,Liu, Wei,Tan, Shanlun,Cai, Zhan,Ni, Tingjunhong,An, Maomao,Li, Ran,Gao, Yue,Zhang, Dazhi,Jiang, Yuanying
, p. 34 - 37 (2015/02/19)
A series of caffeic acid amides were designed, synthesized, and their synergistic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The title caffeic acid amides 3-30 except 26 exhibited potent activity, and the subsequent SAR study was conducted. Compound 3, 5, 21, and 34c, at a concentration of 1.0 μg/ml, decreased the MIC80 of fluconazole from 128.0 μg/ml to 1.0-0.5 μg/ml against the fluconazole-resistant C. albicans. This result suggests that the caffeic acid amides, as synergists, can sensitize drug-resistant fungi to fluconazole. The SAR study indicated that the dihydroxyl groups and the amido groups linking to phenyl or heterocyclic rings are the important pharmacophores of the caffeic acid amides.
Synthesis of hexahydrocyclopenta[ ij ]isoquinolines as a new class of dopaminergic agents
Prraga, Javier,Galn, Abraham,Sanz, Maria Jess,Cabedo, Nuria,Cortes, Diego
, p. 101 - 106 (2015/01/08)
In this study, we have described the synthesis of the tricyclic 1,2,3,7,8,8a-hexahydrocyclopenta [ij]isoquinoline (HCPIQ). Herein, six differently substituted 5,6-dioxygenated-7-phenyl-HCPIQs have been synthesized using a new methodology via (E)-1-styryl-
Synthesis of hexahydrocyclopenta[ ij[isoquinolines as a new class of dopaminergic agents
Párraga, Javier,Galán, Abraham,Sanz, Maria Jesús,Cabedo, Nuria,Cortes, Diego
, p. 101 - 106 (2015/05/26)
In this study, we have described the synthesis of the tricyclic 1,2,3,7,8,8a-hexahydrocyclopenta [ij]isoquinoline (HCPIQ). Herein, six differently substituted 5,6-dioxygenated-7-phenyl-HCPIQs have been synthesized using a new methodology via (E)-1-styryl-
Synthesis and antihyperglycemic activity of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines
Dwivedi, Atma P.,Kumar, Shailesh,Varshney, Vandana,Singh, Amar B.,Srivastava, Arvind K.,Sahu, Devi P.
, p. 2301 - 2305 (2008/09/21)
A series of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines were synthesized and evaluated for their antihyperglycemic activity. Compounds 3g and 6d exhibited lowering of postprandial plasma glucose by 30.7%, 23.3% in SLM and 25.6%, 25.4% in STZ models respectively which is significant compared to metformin and glybenclamide. Other compounds exhibited moderate to good activity ranging from 19.5% to 32.8% in SLM and 3.26% to 25.4% in STZ models.
A novel [2 + 2] photodimerization of N-[(E)-3,4-methylenedioxycinnamoyl]dopamine in the solid state.
Ito,Horie,Shindo
, p. 2411 - 2413 (2007/10/03)
[reaction: see text] To give photoreactivity to catecholamines, N-cinnamoyl-substituted dopamines (E)-5a-5c and O,O'-dimethyldopamines (E)-3a-3c were prepared under solvent-free conditions. A particularly interesting observed photoreactivity was that of N-[(E)-3,4-methylenedioxycinnamoyl]dopamine ((E)-5c), which underwent a novel type of [2 + 2] photodimerization in the solid state, giving exclusively a tricyclic product 8. This reaction is the first example of solid-state photoaddition of an alkene to the benzene ring.
