- New pyrazole derivatives as CRAC channel modulators
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The present invention relates to compounds of formula (I) which are inhibitors of CRAC channel activity. This invention also relates to pharmaceutical compositions containing them, process for their preparation and their use in therapy.
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Paragraph 0099
(2015/03/28)
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- Targeting the human parasite Leishmania donovani: Discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series
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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.
- 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
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p. 7155 - 7164
(2013/11/06)
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- 3-Benzamido, ureido and thioureidoimidazo[1,2-a]pyridine derivatives as potential antiviral agents
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This work reports the synthesis and the antiviral activities of 3-benzamido, 3-phenylureido and 3-phenylthioureido derivatives in the imidazo[1,2-a]pyridine series. The structure was proven by NMR spectroscopy. The synthesized compounds were evaluated against a large number of viruses. The 3-phenylthioureido derivative 7 showed moderate activity against human cytomegalovirus (HCMV) in vitro. The crystallographic data for 8 are also reported and explain the absence of activity against human immunodeficiency virus (HIV).
- Chaouni-Benabdallah, Aziz,Galtier, Christophe,Allouchi, Hassan,Kherbeche, Abdelak,Chavignon, Olivier,Teulade, Jean-Claude,Witvrouw, Myriam,Pannecouque, Christophe,Snoeck, Robert,Andrei, Graciela,Balzarini, Jan,De Clercq, Erik,Fauvelle, Florence,Enguehard, Cecile,Gueiffier, Alain
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p. 1631 - 1635
(2007/10/03)
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- Chemotherapeutically effective nitro compounds. III. Nitropyridines, nitroimidazopyridines and related compounds
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New 2 nitropyridines and 3 nitropyridines, and 3 nitroimidazo [1,2 a] pyridines and related compounds (together 106) were synthesized and tested for their chemotherapeutic efficacy against trichomonads, amoebas and other organisms, such as Eimeria tenella, bacteria, fungi and helminths. Several 2 nitropyridines revealed a detectable systemic effect against Entamoeba histolytica (extraintestinal amoebiasis of the golden hamster) and also a weak activity against Trichomonas fetus in the NMRI mouse. Only a few 3 nitropyridines showed a marked systemic effect against trichomonads. Of the 3 nitroimidazo [1,2 a] pyridines, only the electroneutral carboxylic acid amide group exhibited a pronounced activity, exclusively against trichomonads; however, the activity was nullified by electronegative, electropositive and other electroneutral substituents. As they were not superior in chemotherapeutic respect compared to the known standard preparations (metronidazole), no further tests were carried out with the most effective compounds.
- Winkelmann,Raether,Hartung,Wagner
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