885275-91-2Relevant academic research and scientific papers
HETEROAROMATIC COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF
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Paragraph 0310; 0311; 0312, (2014/11/11)
The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
DIAMINOPYRAZINE COMPOUNDS, MEDICAMENTS CONTAINING SAID COMPOUNDS, USE THEREOF AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 42, (2014/11/13)
The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
Targeting the human parasite Leishmania donovani: Discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series
Castera-Ducros, Caroline,Paloque, Lucie,Verhaeghe, Pierre,Casanova, Magali,Cantelli, Christophe,Hutter, Sébastien,Tanguy, Floriane,Laget, Michèle,Remusat, Vincent,Cohen, Anita,Crozet, Maxime D.,Rathelot, Pascal,Azas, Nadine,Vanelle, Patrice
, p. 7155 - 7164 (2013/11/06)
We report herein the discovery of antileishmanial molecules based on the imidazo[1,2-a]pyridine ring. In vitro screenings of imidazopyridines belonging to our chemical library, toward the promastigotes stage of Leishmania donovani, J774A.1 murine and HepG2 human cells, permitted to identify three selective hit-compounds (12, 20 and 28). New derivatives were then synthesized to allow structure-activity and -toxicity relationships analyses, enabling to characterize a lead-compound (44) displaying both a high potency (IC 50 = 1.8 μM) and a good selectivity index, in comparison with three antileishmanial reference drug-compounds (amphotericin B, miltefosine and pentamidine). Moreover, lead-compound 44 also exhibits good in vitro activity against the intracellular amastigote stage of L. donovani. Thus, the 6-halo-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridine scaffold appears as a new promising selective antileishmanial pharmacophore, especially when substituted at position 8 by a bromine atom.
2-[(4-Phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D 4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl) piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist
Enguehard-Gueiffier, Cécile,Hübner, Harald,El Hakmaoui, Ahmed,Allouchi, Hassan,Gmeiner, Peter,Argiolas, Antonio,Melis, Maria Rosaria,Gueiffier, Alain
, p. 3938 - 3947 (2007/10/03)
A series of novel 2-[(4-phenylpiperazin-1-yl)methyl]imidazoazines and aza-analogues were prepared and screened at selected dopamine, serotonin, and adrenergic receptor subtypes. 2-Substituted imidazopyridines and pyridazines presented high affinities and
