137643-31-3Relevant academic research and scientific papers
Indole-based heterocyclic inhibitors of p38α MAP kinase: Designing a conformationally restricted analogue
Mavunkel, Babu J.,Chakravarty, Sarvajit,Perumattam, John J.,Luedtke, Gregory R.,Liang, Xi,Lim, Don,Xu, Yong-Jin,Laney, Maureen,Liu, David Y.,Schreiner, George F.,Lewicki, John A.,Dugar, Sundeep
, p. 3087 - 3090 (2003)
p38α Mitogen Activated Protein Kinase (MAP kinase) is an intracellular soluble serine threonine kinase. p38α kinase is activated in response to cellular stresses, growth factors and cytokines such as interleukin-1 (IL-1) and tumor necrosis factor alpha (TNF-α). The central role of p38α activation in settings of both chronic and acute inflammation has led efforts to find inhibitors of this enzyme as possible therapies for diseases such as rheumatoid arthritis, where p38α activation is thought to play a causal role. Herein, we report structure-activity relationship studies on a series of indole-based heterocyclic inhibitors that led to the design and identification of a new class of p38α inhibitors.
Acylative Coupling of Amine and Indole Using Chloroform as a Carbonyl Group
Nishida, Yuika,Takeda, Norihiko,Matsuno, Kenji,Miyata, Okiko,Ueda, Masafumi
, p. 3928 - 3935 (2018/07/31)
Chloroform-mediated acylative coupling of amines with indoles has been developed. When indoles and amines in chloroform were treated with dimethylzinc in the presence of air, the three-component aminocarbonylation reaction proceeded via in-situ generation of phosgene from chloroform and O2 to provide indole-3-carboxamides in a single operation. Application to the synthesis of biologically active compounds and intramolecular acylation are also described.
AlMe3-mediated regio- and chemoselective reactions of indole with carbamoyl electrophiles
Velavan,Sumathi,Balasubramanian
, p. 3148 - 3157 (2013/06/27)
Herein, we report the regio- and chemoselective reactions of indole with carbamoyl electrophiles in presence of AlMe3. Indole-3-carboxamide was prepared in one-step from a reaction of indole with tertiary carbamoylimidazole in the presence AlMe
