27423-83-2Relevant academic research and scientific papers
Isoform-selective inhibitory profile of 2-imidazoline-substituted benzene sulfonamides against a panel of human carbonic anhydrases
Supuran, Claudiu T.,Kalinin, Stanislav,Tan?, Muhammet,Sarnpitak, Pakornwit,Mujumdar, Prashant,Poulsen, Sally-Ann,Krasavin, Mikhail
, p. 197 - 202 (2016/12/03)
A series of novel benzene sulfonamides (previously evaluated as selective cyclooxygenase-2 inhibitors) has been profiled against human carbonic anhydrases I, II, IV and VII in an attempt to observe the manifestation of the well established “tail” approach
Reactions of some ortho and para halogenated aromatic nitriles with ethylenediamine: Selective synthesis of imidazolines
Crane, Louis J.,Anastassiadou, Maria,Stigliani, Jean-Luc,Baziard-Mouysset, Geneviève,Payard, Marc
, p. 5325 - 5330 (2007/10/03)
The reaction of ethylenediamine (EDA) with ortho and/or para halogenated benzonitriles did not lead to the imidazolines expected: a competitive aromatic nucleophilic substitution (SNAr) was observed instead. The selective synthesis of these imidazolines was performed by nucleophilic addition of EDA to thiobenzamide derivatives. The difference in reactivity between the nitrile and thioamide derivatives was estimated by a frontier orbital approach at the RHF/6-31G** level which predicted a greater reactivity of substituted thiobenzamides towards the nucleophilic addition of EDA.
Synthesis and pharmacological evaluation of imidazoline sites I1 and I2 selective ligands
Anastassiadou, Maria,Danoun, Sada,Crane, Louis,Baziard-Mouysset, Genevieve,Payard, Marc,Caignard, Daniel-Henri,Rettori, Marie-Claire,Renard, Pierre
, p. 585 - 592 (2007/10/03)
Several series of 2-aryl or heterocyclic-imidazoline compounds have been prepared and evaluated in vitro as imidazoline sites (I1 and I2) and α-adrenergic (α1 and α2) receptor ligands. Their pKi values indicate that linkage of the imidazoline moiety at the 2-position with an aromatic substituent dramatically decreases α-adrenergic affinity. I1 sites are more accessible by phenyl imidazolines substituted by a methyl or a methoxy group at the ortho or meta position. Indeed, 2-(2′-methoxyphenyl)-imidazoline (17) is one of the best I1 ligands ever reported (pKi=8.53 and I1/I2>3388). On the other hand, I2 selectivity increases in the presence of a methyl group in the para position. The original compound, 2-(3′-fluoro-4′-tolyl)-imidazoline (31) is a new potent ligand for the I2 sites with high selectivity (pKi=8.53 and I2/I1>3388). Copyright
