213680-53-6Relevant academic research and scientific papers
Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia
Regenass, Pierre,Abboud, Dayana,Daubeuf, Fran?ois,Lehalle, Christine,Gizzi, Patrick,Riché, Stéphanie,Hachet-Haas, Muriel,Rohmer, Fran?ois,Gasparik, Vincent,Boeglin, Damien,Haiech, Jacques,Knehans, Tim,Rognan, Didier,Heissler, Denis,Marsol, Claire,Villa, Pascal,Galzi, Jean-Luc,Hibert, Marcel,Frossard, Nelly,Bonnet, Dominique
supporting information, p. 7671 - 7686 (2018/09/06)
We previously reported Chalcone-4 (1) that binds the chemokine CXCL12, not its cognate receptors CXCR4 or CXCR7, and neutralizes its biological activity. However, this neutraligand suffers from limitations such as poor chemical stability, solubility, and oral activity. Herein, we report on the discovery of pyrimidinone 57 (LIT-927), a novel neutraligand of CXCL12 which displays a higher solubility than 1 and is no longer a Michael acceptor. While both 1 and 57 reduce eosinophil recruitment in a murine model of allergic airway hypereosinophilia, 57 is the only one to display inhibitory activity following oral administration. Thereby, we here describe 57 as the first orally active CXCL12 neutraligand with anti-inflammatory properties. Combined with a high binding selectivity for CXCL12 over other chemokines, 57 represents a powerful pharmacological tool to investigate CXCL12 physiology in vivo and to explore the activity of chemokine neutralization in inflammatory and related diseases.
Inhibiting Firefly Bioluminescence by Chalcones
Zhang, Huateng,Su, Jing,Lin, Yuxin,Bai, Haixiu,Liu, Jiaxiang,Chen, Hui,Du, Lupei,Gu, Lichuan,Li, Minyong
, p. 6099 - 6105 (2017/06/23)
Chalcone refers to an aromatic ketone and an enone that constitutes the central core for various important biological compounds in drug discovery. Moreover, the firefly luciferase (Fluc) as the bioluminescent reporter has been widely used in life science
Pyridines and pyrazolines from salicylic acid derivatives with propenone residue and their antimicrobial properties
Grant,Mishriky,Asaad,Fawzy
, p. 543 - 547 (2007/10/03)
Reaction of the propenones 1c, d with chlorosulfonyl isocyanate followed by hydrolysis gave the corresponding carbamoyloxybenzoates 2a, b. While their reaction with ethyl isocyanate afforded the 1,3-benzoxazine-2,4-diones 3a, b. Reaction of 1a, b with aryl hydrazines gave the pyrazolines 4a, d, whereas, with hydrazine hydrate in acetic acid, the acetyl derivatives 4e, f were produced. 1c, d reacted with malononitrile and ethyl cyanoacetate affording the cyanopyridines 5 and cyanopyridones 6 respectively. The products show antimicrobial activities.
