104863-69-6Relevant articles and documents
α-Ketoheterocycles Able to Inhibit the Generation of Prostaglandin E2 (PGE2) in Rat Mesangial Cells
Psarra, Anastasia,Theodoropoulou, Maria A.,Erhardt, Martin,Mertiri, Marina,Mantzourani, Christiana,Vasilakaki, Sofia,Magrioti, Victoria,Huwiler, Andrea,Kokotos, George
, p. 1 - 19 (2021)
Prostaglandin E2 (PGE2 ) is a key mediator of inflammation, and consequently huge efforts have been devoted to the development of novel agents able to regulate its formation. In this work, we present the synthesis of various α-ketoheterocycles and a study of their ability to inhibit the formation of PGE2 at a cellular level. A series of α-ketobenzothiazoles, α-ketobenzoxazoles, α-ketobenzimidazoles, and α-keto-1,2,4-oxadiazoles were synthesized and chemically characterized. Evaluation of their ability to suppress the generation of PGE2 in interleukin-1β plus forskolinstimulated mesangial cells led to the identification of one α-ketobenzothiazole (GK181) and one α-ketobenzoxazole (GK491), which are able to suppress the PGE2 generation at a nanomolar level.
Expedient synthesis of 3-alkoxymethyl- And 3-aminomethyl-pyrazolo[3,4-b] pyridines
Beutner, Gregory L.,Kuethe, Jeffrey T.,Kim, Mary M.,Yasuda, Nobuyoshi
supporting information; experimental part, p. 789 - 794 (2009/06/20)
An effective strategy has been developed for the preparation of 3-alkoxymethyl-pyrazolo[3,4-b]pyridines, compounds that are currently not readily accessible by existing synthetic methods. Further manipulation of these compounds allows for access to 3-alkoxymethyl-pyrazolo[3,4-b]pyridines with a variety of substitution patterns as well as 3-aminomethyl-pyrazolo[3,4-b] pyridines.
