182181-25-5Relevant articles and documents
HETEROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF AMYLOID-RELATED DISEASES
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Paragraph 0186, (2020/08/28)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
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.
IMIDAZO[1,2-A]PYRIDINES FOR THE TREATMENT OF CNS AND CARDIAC DISEASES
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, (2008/06/13)
The present invention relates to imidazo[1,2-a]pyridine compounds of formula (1) STR1 which are dopamine D-4 antagonists and useful as anti-psychotic agents.