@article{3076733,
    title = "α-Ketoheterocycles Able to Inhibit the Generation of Prostaglandin E2 (PGE2) in Rat Mesangial Cells",
    author = "Psarra, A. and Theodoropoulou, M.A. and Erhardt, M. and Mertiri, M. and Mantzourani, C. and Vasilakaki, S. and Magrioti, V. and Huwiler, A. and Kokotos, G.",
    journal = "Ancient Biomolecules",
    year = "2021",
    volume = "11",
    number = "2",
    pages = "1-19",
    publisher = "MDPI AG",
    issn = "1358-6122",
    doi = "10.3390/biom11020275",
    keywords = "alfacalcidol;  benzimidazole derivative;  benzothiazole;  casein kinase II;  chemical compound;  cyanohydrin;  drug metabolite;  essential oil;  interleukin 1beta;  oxadiazole derivative;  prostaglandin E2;  terpene;  tetrabutylammonium;  heterocyclic compound;  prostaglandin E2;  prostaglandin receptor blocking agent, animal cell;  animal experiment;  antineoplastic activity;  Article;  Candida albicans;  carbon nuclear magnetic resonance;  controlled study;  crystal structure;  crystallization;  drug synthesis;  EC50;  enzyme active site;  enzyme inhibition;  human;  hydrodistillation;  IC50;  inflammation;  infrared spectroscopy;  lipophilicity;  mass fragmentography;  mass spectrometry;  mesangium cell;  molecular docking;  Mycobacterium tuberculosis;  nonhuman;  physical chemistry;  proton nuclear magnetic resonance;  structure activity relation;  thin layer chromatography;  X ray crystallography;  animal;  biosynthesis;  cell culture;  cytology;  drug effect;  mesangium;  metabolism;  procedures;  rat;  spectroscopy, Animals;  Cells, Cultured;  Dinoprostone;  Glomerular Mesangium;  Heterocyclic Compounds;  Molecular Docking Simulation;  Prostaglandin Antagonists;  Rats;  Spectrum Analysis",
    abstract = "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. © 2021 by the authors. Licensee MDPI, Basel, Switzerland."
}