207982-87-4Relevant articles and documents
Antimycobacterial activity of 5-arylidene aromatic derivatives of hydantoin
Szymanska, Ewa,Kiec-Kononowicz, Katarzyna
, p. 355 - 362 (2002)
Various 5-(chlorobenzylidene)-2-isoniazido and 5-(chlorobenzylidene)-2-amino substituted derivatives of imidazoline-4-one were synthesized and evaluated in the primary assay for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Eight of them exhibited >90% inhibition in the primary screening at 12.5 μg/ml. For these primarily selected compounds the actual MIC and IC50 values were determined. Two of the isoniazid derivatives, for which MIC≤3.13 μg/ml and SI>10, were selected for further screening and investigated for efficacy in vitro in a TB-infected macrophage model. The most promising compound, 5-(3-chlorobenzylidene)-2-(isonicotinoylhydrazino)-imidazoline-4-one, with activity in vitro comparable with rifampin (MIC=0.8 μg/ml, SI>78) was tested in vivo in the animal tuberculosis model but exhibited insignificant activity. For several compounds the primary screening of antimycobacterial activity against Mycobacterium avium (ATCC 25291) was conducted as well, but none of them demonstrated satisfactory activity.
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
Synthesis of 5-arylidene-2-amino-4-azolones and evaluation of their anticancer activity
Subtel'Na, Ivanna,Atamanyuk, Dmytro,Szymanska, Ewa,Kiec-Kononowicz, Katarzyna,Zimenkovsky, Borys,Vasylenko, Olexandr,Gzella, Andrzej,Lesyk, Roman
experimental part, p. 5090 - 5102 (2010/09/06)
Series of novel 5-arylidene-2-arylaminothiazol-4(5H)-ones and 2-aryl(benzyl)amino-1H-imidazol-4(5H)-ones were synthesized from appropriate 2-alkylthioazol-4-ones using nucleophilic substitution in position 2 by various anilines and benzylamines and Knoeve
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.
Structure and activity studies of glycine receptor ligands. Part 7. Structural remarks on arylidene-imidazoline-4-one glycinates and glycinamides
Karolak-Wojciechowska, Janina,Kie?-Kononowicz, Katarzyna,Mrozek, Agnieszka
, p. 73 - 81 (2007/10/03)
To improve the physicochemical properties (lipophilicity) of the potential ligands of glycine binding site of NMDA receptor, esters and amides of glycine derivatives of arylidene-imidazolidine-4-ones were obtained. The analysis of their properties (X-ray crystallography, NMR spectral data and theoretical calculations) was performed with respect to the existence of the probable tautomeric forms. Their possible interaction with hypothetical active points of the receptor (taking into the account the model of glycine binding site of NMDA receptor) was discussed on the basis of simulation with IsoStar. program.
Synthesis, conformational analysis and antitumor testing of 5-(Z)-arylidene-4-imidazolidinone derivatives
Khodair,El-Subbagh,Al-Obaid
, p. 159 - 181 (2007/10/03)
A series of 5-(Z)-arylidene-2-amino-4-imidazolidinones 16-34, 5-(Z)-arylidene-2-(2-carboxyphenylamino)-4-imidazolidinones 35-41, 5-(Z)-arylidene-3-aminomethyl-2-thioxo-4-imidazolidinones 42-55 and 5-(Z)-arylidene-3-aminomethyl-2-methylmercapto-4-imidazoli
