784183-57-9Relevant academic research and scientific papers
Efficient and Divergent Synthesis of Medium-Sized Lactams through Zinc-Catalyzed Oxidative Cyclization of Indoly Ynamides?
Li, Hang-Hao,Ye, Si-Han,Chen, Yang-Bo,Luo, Wen-Feng,Qian, Peng-Cheng,Ye, Long-Wu
supporting information, p. 263 - 268 (2020/02/05)
An efficient zinc-catalyzed oxidative cyclization of readily available indoly ynamides has been developed, enabling rapid and practical access to a diverse array of valuable medium-sized lactams in mostly good to excellent yields with wide substrate scope. In addition, such an asymmetric synthesis has also been explored by employing the chiral substrate.
Spiro heterocycles as potential inhibitors of SIRT1: Pd/C-mediated synthesis of novel N-indolylmethyl spiroindoline-3,2′-quinazolines
Rambabu,Raja, Guttikonda,Yogi Sreenivas,Seerapu,Lalith Kumar,Deora, Girdhar Singh,Haldar, Devyani,Rao, M.V.Basaveswara,Pal, Manojit
, p. 1351 - 1357 (2013/03/14)
Novel N-indolylmethyl substituted spiroindoline-3,2′-quinazolines were designed as potential inhibitiors of SIRT1. These compounds were synthesized in good yields by using Pd/C-Cu mediated coupling-cyclization strategy as a key step involving the reaction of 1-(prop-2-ynyl)-1′H- spiro[indoline-3,2′-quinazoline]-2,4′(3′H)-dione with 2-iodoanilides. Some of the compounds synthesized have shown encouraging inhibition of Sir 2 protein (a yeast homologue of mammalian SIRT1) in vitro and three of them showed dose dependent inhibition of Sir 2. The docking results suggested that the benzene ring of 1,2,3,4-tetrahydroquinazolin ring system of these molecules occupied the deep hydrophobic pocket of the protein and one of the NH along with the sulfonyl group participated in strong H-bonding interaction with the amino acid residues.
Use of Indole Derivatives as Nurr-1 Activators for the Application Thereof as a Medicament for the Treatment of Parkinson's Disease
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Page/Page column 37, (2012/09/22)
Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.
Pd/C-Mediated synthesis of indoles in water
Layek, Mohosin,Lakshmi, Udaya,Kalita, Dipak,Barange, Deepak K.,Islam, Aminul,Mukkanti, K.,Pal, Manojit
experimental part, (2010/04/22)
We describe the utility of a Pd/C-Cu mediated method in the synthesis of 2,s 5-disubstituted indoles in water via a coupling-cyclization strategy. Further application of this methodology has been demonstrated in the preparation of a target indole derivative via a 7-step process the key step being the Pd/C-mediated coupling reaction.
A bioisosteric approach to the discovery of indole carbinol androgen receptor ligands
Lanter, James C.,Fiordeliso, James J.,Allan, George F.,Musto, Amy,Hahn, Do Won,Sui, Zhihua
, p. 5646 - 5649 (2007/10/03)
Two potential bioisosteres of the nonsteroidal antiandrogen bicalutamide, an imidazolidinone and an indole, were synthesized and tested for their androgen receptor binding. Indole was discovered to be a suitable bioisostere for the acyl anilide moiety in the parent compound. Several analogs in the indole series were found to be 10-fold better than bicalutamide in binding to the recombinant androgen receptor binding domain.
