1489263-03-7Relevant academic research and scientific papers
KI-Promoted Oxidative Coupling of Styrenes with Indoles under Metal-Free Conditions: Facile Access to C-3 Dicarbonyl Indoles
Fang, Zheng,Guo, Kai,Guo, Shiyu,He, Wei,Li, Xin,Liu, Chengkou,Yang, Zhao,Zhou, Bochao,Zhu, Ning
, p. 3511 - 3519 (2019)
A new and efficient method for the synthesis of C-3 dicarbonyl indoles via oxidative cross-coupling of styrenes with indoles under metal-free conditions has been developed. Moreover, a broad scope of C-3 dicarbonyl indoles in moderate to good yields were obtained, and a plausible mechanism is proposed based on control and isotope-labeling experiments.
Synthesis method of double-carbonyl indole compounds
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Paragraph 0087-0090, (2018/12/13)
The invention discloses a synthesis method of double-carbonyl indole compounds. The synthesis method comprises the following steps of performing oxidization coupling reaction on acetaldehyde derivatives I and indole derivatives II to obtain the double-car
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives
Taliani, Sabrina,Trincavelli, Maria Letizia,Cosimelli, Barbara,Laneri, Sonia,Severi, Elda,Barresi, Elisabetta,Pugliesi, Isabella,Daniele, Simona,Giacomelli, Chiara,Greco, Giovanni,Novellino, Ettore,Martini, Claudia,Da Settimo, Federico
, p. 331 - 337 (2013/10/21)
We have disclosed a series of 1-benzyl-3-ketoindole derivatives acting as either positive or negative modulators of the human A2B adenosine receptor (A2B AR) depending on small differences in their side chain. The new compounds were designed taking into account structural similarities between AR antagonists and ligands of the GABAA/benzodiazepine receptor. All compounds resulted totally inactive at A2A and A 3 ARs and showed small (8a,b) or none (7a,b, 8c and 9a,b) affinity for A1 AR. When tested on A2B AR-transfected CHO cells, 7a,b and 8a acted as positive modulators, whereas 8b,c and 9a,b acted as negative modulators, enhancing or weakening the NECA-induced increase of cAMP levels, respectively. Compounds 7-9 might be regarded as useful biological and pharmacological tools to explore the therapeutic potential of A2B AR modulators, while their 3-ketoindole scaffold might be taken as a reference to design new analogs.
