1809028-84-9Relevant articles and documents
in Water : Organocatalyzed Diastereoselective Multicomponent Reactions toward 2-Azapyrrolizidine Alkaloid Scaffolds
Rajarathinam, Balakrishnan,Kumaravel, Kandhasamy,Vasuki, Gnanasambandam
, p. 455 - 463 (2017)
Synthesis of the 2-aza analogues of pyrrolizidine and spirooxindole-2-azapyrrolizidine hybrid, a spiro-tetracyclic scaffold possessing multiple contiguous stereocenters, by an exclusive regio-, chemo-, and diastereoselective multicomponent reaction in water is reported. This logical and didactical tactic has integrated the principles of an ideal organic synthesis, privileged substructure-based diversity-oriented synthesis, and biology-oriented synthesis to access hybrid heterocyclic scaffolds.
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.
5-Arylideneimidazolones with amine at position 3 as potential antibiotic adjuvants against multidrug resistant bacteria
Kaczor, Aneta,Witek, Karolina,Podlewska, Sabina,Czekajewska, Joanna,Lubelska, Annamaria,Zes?awska, Ewa,Nitek, Wojciech,Latacz, Gniewomir,Alibert, Sandrine,Pagès, Jean-Marie,Karczewska, Elzbieta,Kie?-Kononowicz, Katarzyna,Handzlik, Jadwiga
, (2019/01/30)
Searching for new chemosensitizers of bacterial multidrug resistance (MDR), chemical modifications of (Z)-5-(4-chlorobenzylidene)-2-(4-methylpiperazin-1-yl)-3H-imidazol-4(5H)-one (6) were performed. New compounds (7–17), with fused aromatic rings at posit