95474-44-5Relevant articles and documents
Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors
Ahn, Kwang H.,Bazureau, Jean-Pierre,Burgy, Guillaume,Deau, Emmanuel,Durieu, Emilie,Fant, Xavier,Herault, Yann,Kendall, Debra A.,Khurana, Leepakshi,L'Helgoual'Ch, Jean-Martial,Limanton, Emmanuelle,Lindberg, Mattias F.,Meijer, Laurent,Nguyen, Thu Lan,Roche, Didier,Tahtouh, Tania,Bruyère, Céline,Carreaux, Fran?ois,Guiheneuf, Solène,Miege, Frédéric,Sévère, Elodie,Villiers, Beno?t
supporting information, (2022/01/03)
The protein kinase DYRK1A is involved in Alzheimer's disease, Down syndrome, diabetes, viral infections, and leukemia. Leucettines, a family of 2-aminoimidazolin-4-ones derived from the marine sponge alkaloid Leucettamine B, have been developed as pharmacological inhibitors of DYRKs (dual specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like kinases). We report here on the synthesis and structure-activity relationship (SAR) of 68 Leucettines. Leucettines were tested on 11 purified kinases and in 5 cellular assays: (1) CLK1 pre-mRNA splicing, (2) Threonine-212-Tau phosphorylation, (3) glutamate-induced cell death, (4) autophagy and (5) antagonism of ligand-activated cannabinoid receptor CB1. The Leucettine SAR observed for DYRK1A is essentially identical for CLK1, CLK4, DYRK1B, and DYRK2. DYRK3 and CLK3 are less sensitive to Leucettines. In contrast, the cellular SAR highlights correlations between inhibition of specific kinase targets and some but not all cellular effects. Leucettines deserve further development as potential therapeutics against various diseases on the basis of their molecular targets and cellular effects.
Sulfated and Oxygenated Imidazoline Derivatives: Synthesis, Antioxidant Activity and Light-Mediated Antibacterial Activity
Alves Borges Leal, Antonio L.,Barreto, Humberto M.,Faillace, Martín S.,Muratori da Costa, Luciana,Peláez, Walter J.,Silva, Ana P.
, (2020/04/15)
Imidazoline derivatives with different exocyclic substituents were simply prepared from common starting materials. The procedures were carried out in an eco-friendly manner. The antioxidant activity of these derivatives was explored by different experimental assays, such as ABTS.+ and DPPH. scavenging assay, as well as reducing power assay. The structural differences are discussed in terms of the results. Sulfur analogs showed higher antioxidant activity than their oxygenated counterparts. The same tendency was observed in microbiological studies, in which the same imidazoline compounds were assayed for light-mediated activity against of Staphylococcus aureus and Escherichia coli strains. A light-enhanced activity was observed for almost all the sulfated imidazolines after exposure to UV-A (400-320 nm) light.
Bicyclic imidazole-4-one derivatives: A new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55
Rempel,Atzler,Behrenswerth,Karcz,Schoeder,Hinz,Kaleta,Thimm,Kiec-Kononowicz,Müller
, p. 632 - 649 (2014/05/06)
GPR18 and GPR55 are orphan G protein-coupled receptors (GPCRs) that interact with certain cannabinoid (CB) receptor ligands. In the present study bicyclic imidazole-4-one derivatives were discovered as new scaffolds for the development of antagonists for
