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

被引：1
|
作者：
Psarra, Anastasia [1 ]
Theodoropoulou, Maria A. [1 ]
Erhardt, Martin [2 ]
Mertiri, Marina [1 ]
Mantzourani, Christiana [1 ]
Vasilakaki, Sofia [1 ]
Magrioti, Victoria [1 ]
Huwiler, Andrea [2 ]
Kokotos, George [1 ]
机构：
[1] Natl & Kapodistrian Univ Athens, Dept Chem, Athens 15771, Greece
[2] Univ Bern, Inst Pharmacol, CH-3010 Bern, Switzerland
来源：
BIOMOLECULES | 2021年 / 11卷 / 02期
基金：
瑞士国家科学基金会;
关键词：
anti-inflammatory; inhibition; alpha-ketobenzothiazoles; mesangial cells; prostaglandin E-2;
D O I：
10.3390/biom11020275
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Prostaglandin E-2 (PGE(2)) 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 alpha-ketoheterocycles and a study of their ability to inhibit the formation of PGE(2) at a cellular level. A series of alpha-ketobenzothiazoles, alpha-ketobenzoxazoles, alpha-ketobenzimidazoles, and alpha-keto-1,2,4-oxadiazoles were synthesized and chemically characterized. Evaluation of their ability to suppress the generation of PGE(2) in interleukin-1 beta plus forskolin-stimulated mesangial cells led to the identification of one alpha-ketobenzothiazole (GK181) and one alpha-ketobenzoxazole (GK491), which are able to suppress the PGE(2) generation at a nanomolar level.
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页码：1 / 19
页数：19
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