α-Ketoheterocycles Able to Inhibit the Generation of Prostaglandin E2 (PGE2) in Rat Mesangial Cells.

Anastasia Psarra, Maria A Theodoropoulou, Martin Erhardt, Marina Mertiri, Christiana Mantzourani, Sofia Vasilakaki, Victoria Magrioti, Andrea Huwiler, George Kokotos

Biomolecules 2021 Feb 13

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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 forskolin-stimulated 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.

Citation

Anastasia Psarra, Maria A Theodoropoulou, Martin Erhardt, Marina Mertiri, Christiana Mantzourani, Sofia Vasilakaki, Victoria Magrioti, Andrea Huwiler, George Kokotos. α-Ketoheterocycles Able to Inhibit the Generation of Prostaglandin E2 (PGE2) in Rat Mesangial Cells. Biomolecules. 2021 Feb 13;11(2)