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 (2021). α-Ketoheterocycles Able to Inhibit the Generation of Prostaglandin E2 (PGE2) in Rat Mesangial Cells. Biomolecules, 11(2) MDPI 10.3390/biom11020275

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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.

Item Type:

Journal Article (Original Article)

Division/Institute:

04 Faculty of Medicine > Pre-clinic Human Medicine > Institute of Pharmacology

UniBE Contributor:

Erhardt, Martin and Huwiler, Andrea

Subjects:

600 Technology > 610 Medicine & health

ISSN:

2218-273X

Publisher:

MDPI

Language:

English

Submitter:

Celine Joray

Date Deposited:

06 Apr 2021 11:52

Last Modified:

07 Apr 2021 01:34

Publisher DOI:

10.3390/biom11020275

PubMed ID:

33668480

Uncontrolled Keywords:

anti-inflammatory inhibition mesangial cells prostaglandin E2 α-ketobenzothiazoles

BORIS DOI:

10.48350/155532

URI:

https://boris.unibe.ch/id/eprint/155532

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