73031-16-0Relevant articles and documents
Novel positive allosteric modulators of A2B adenosine receptor acting as bone mineralisation promoters
Barresi, Elisabetta,Giacomelli, Chiara,Marchetti, Laura,Baglini, Emma,Salerno, Silvia,Greco, Giovanni,Da Settimo, Federico,Martini, Claudia,Trincavelli, Maria Letizia,Taliani, Sabrina
, p. 286 - 294 (2021)
Small-molecules acting as positive allosteric modulators (PAMs) of the A2B adenosine receptor (A2B AR) could potentially represent a novel therapeutic strategy for pathological conditions characterised by altered bone homeostasis, including osteoporosis. We investigated a library of compounds (4-13) exhibiting different degrees of chemical similarity with three indole derivatives (1-3), which have been recently identified by us as PAMs of the A2B AR able to promote mesenchymal stem cell differentiation and bone formation. Evaluation of mineralisation activity of 4-13 in the presence and in the absence of the agonist BAY60-6583 allowed the identification of lead compounds with therapeutic potential as anti-osteoporosis agents. Further biological characterisation of one of the most performing compounds, the benzofurane derivative 9, confirmed that such a molecule behaves as PAM of the A2B AR.
Synthesis of α-ketoamides using potassium superoxide (KO2) as an oxidizing agent
Vasudevan,Routholla, Ganesh,Teja Illa, Giri,Reddy, D. Srinivasa
, (2020/05/25)
A simple and convenient method for the synthesis of α-ketoamides by the oxidation of aryl acetamides using potassium superoxide (KO2) as an oxidizing agent is disclosed here. The scope of the developed method is successfully tested with fifteen substrates. In addition, the utility of method has been demonstrated by synthesizing an orexin receptor antagonist, a medicinally interesting compound.
Indole amide synthesis of derivatives and their use as plant growth regulators
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Paragraph 0016-0018, (2019/07/11)
The invention discloses indole amide derivatives and its synthetic method, is to indole, oxalyl, aromatic amine as the main raw material, by conventional solvent method and ultrasonic radiation method for synthesis of a indolyl for the skeleton to amide derivatives. Because the indole amide in the molecule containing both indole group, but also has the amide structure, under the condition of the best concentration demonstrates the role in promoting the growth of wheat, indole acetic acid than more dominating, and therefore as a plant growth regulator is applied to the agricultural production has very good prospects.
