163630-17-9Relevant academic research and scientific papers
Neuroprotective Effect of IND1316, an Indole-Based AMPK Activator, in Animal Models of Huntington Disease
Vela, Marta,García-Gimeno, María Adelaida,Sanchis, Ana,Bono-Yagüe, José,Cumella, José,Lagartera, Laura,Pérez, Concepción,Priego, Eva-María,Campos, Angela,Sanz, Pascual,Vázquez-Manrique, Rafael P.,Castro, Ana
, p. 275 - 287 (2022/01/15)
Aggregation of mutant huntingtin, because of an expanded polyglutamine track, underlies the cause of neurodegeneration in Huntington disease (HD). However, it remains unclear how some alterations at the cellular level lead to specific structural changes in HD brains. In this context, the neuroprotective effect of the activation of AMP-activated protein kinase (AMPK) appears to be a determinant factor in several neurodegenerative diseases, including HD. In the present work, we describe a series of indole-derived compounds able to activate AMPK at the cellular level. By using animal models of HD (both worms and mice), we demonstrate the in vivo efficacy of one of these compounds (IND1316), confirming that it can reduce the neuropathological symptoms of this disease. Taken together, in vivo results and in silico studies of druggability, allow us to suggest that IND1316 could be considered as a promising new lead compound for the treatment of HD and other central nervous system diseases in which the activation of AMPK results in neuroprotection.
INDOLE DERIVATIVES FOR THE PREVENTION AND/OR TREATMENT OF DIABETES AND ASSOCIATED METABOLIC DISORDERS
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Paragraph 0134, (2017/10/26)
The invention relates to substituted heterocyclic indole derivatives of Formula (I), which act as activators of the AMP-activated protein kinase (AMPK) and to the use of them for the treatment and prevention of diseases or disorders regulated by AMPK. As
Palladium-catalyzed annulation of allenes with indole-2-carboxylic acid derivatives: Synthesis of Indolo[2,3-c]pyrane-1-ones via Ar-I Reactivity or C-H functionalization
Suresh, R. Rama,Swamy, K. C. Kumara
experimental part, p. 6959 - 6969 (2012/09/25)
Two methodologies, one involving Ar-I reactivity and the other through C-H functionalization, for the formation of indolo[2,3-c]pyrane-1-ones via the corresponding allenes, are presented. A highly efficient approach to indolo[2,3-c]pyrane-1-one derivatives through the Pd-catalyzed regioselective annulation of allenes with 3-iodo-1-alkylindole-2-carboxylic acids is described. This method is fairly general for a wide range of allenes affording the respective indolo[2,3-c]pyrane-1-ones in good to excellent yields. In addition, a Pd(II)-catalyzed oxidative coupling of indole-2-caboxylic acid derivatives with allenes via direct C-H functionalization to afford the corresponding indolo[2,3-c]pyrane-1-ones in moderate to good yields has been developed.
Regioselective copper-mediated synthesis of thieno[2,3- c ]pyrane-7-one, Indolo[2,3- c ]pyrane-1-one, and indolo[3,2- c ]pyrane-1-one
Inack Ngi, Samuel,Guilloteau, Vincent,Abarbri, Mohamed,Thibonnet, Jerome
supporting information; experimental part, p. 8347 - 8354 (2011/12/04)
In the presence of copper(I) iodide, heteroaromatic Β-iodo-α, Β-unsaturated carboxylic acid systems opposed to terminal alkyne afford selectively 6-endo-dig cyclization products via a tandem coupling oxacyclization reaction.
An expeditious synthesis of structural analogs of the marine cytotoxic agents grossularines-1 and -2
Achab, Said
, p. 2615 - 2618 (2007/10/02)
A short access to 2-carbethoxy-3-(5-imidazolyl)indoles (13, 14, 16), featuring Pd-catalyzed cross coupling between 3-iodoindoles (10-12) and imidazolostannane (9) has been developed. These derivatives when subjected to tandem modified Curtius rearrangement-intramolecular electrocyclization led to the pyridones (19-23) which are key intermediates in the synthesis of the analogs (31), (33) and (36) of the naturally occurring cytotoxic α-carbolines grossularines-1 and -2 (1,2).
