503065-42-7Relevant articles and documents
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
Synthesis and anti-inflammatory activity of some new N and S-alkylated arylidene-thioxo-imidazolidinones
Santos,Mourao,Uchoa,Silva,Malta,Moura,Lima,Galdino,Pitta,Barbe
, p. 433 - 440 (2007/10/03)
New arylidene-thioxo-imidazolidinones and S-alkylated arylidene- imidazolidinone derivatives were prepared from substituted 2-thioxo- imidazolidin-4-one by nucleophilic addition of cyanoacrylates. N and S-alkylation was achieved treating 5-arylidene-2-thi
Structure and activity studies of glycine receptor ligands. Part 8. Arylidene-imidazoline-4-one aminoacids
Karolak-Wojciechowska, Janina,Mrozek, Agnieszka,Kie?-Kononowicz, Katarzyna,Handzlik, Jadwiga
, p. 25 - 36 (2007/10/03)
Based on chemical and preliminary biological experiments (inhibition to glycine receptor), structure and activity relationship of arylidene-imidazoline-4-one amino acids has been studied. In the course of our work, the simulation of the hydrogen bonds formation between ligand molecule and hypothetical receptor has been designed. Computed interactions are going to simulate possible ligand-receptor interaction with selected amino acids (in this investigation - with basic lysine and acidic aspartic acid). Obtained model estimates roughly the binding energy of the amino acids with ligand molecules. The proposed amino acids binding energies approximately agree with activity of the isomeric benzylidene-imidazoline-4-one glycines and α-alanines which decreases in the order of m-Cl > p-Cl > o-Cl substituents in benzylidene moiety. Additionally, the lowering of activity is caused by lipophilic pocket volume.