Alpha Chimica

Châtenay-Malabry, France

Alpha Chimica

Châtenay-Malabry, France

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Abada Z.,University Paris - Sud | Cojean S.,University Paris - Sud | Pomel S.,University Paris - Sud | Ferrie L.,University Paris - Sud | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2013

Importance of heme in African trypanosomes, Leishmania sp. and Plasmodium sp. metabolisms justifies considering the potential of porphyrins and their precursors and derivatives as potential antiparasitic agents by interfering with heme metabolism. Consequently, twenty-four porphyrin precursors and derivatives were evaluated against Leishmania donovani, Trypanosoma brucei and Plasmodium sp. The best active compound against Trypanosoma brucei brucei was a new porphyrin derivative; compound 4i, with a MEC value of 6.25 μM justifying further in vivo evaluation. Whereas these compounds were not active against intramacrophage amastigotes of L. donovani, another new porphyrin derivative, compound 4f was active in vitro against Plasmodium falciparum at 20 nM and a slight delay of mice survival was observed on the Plasmodium berghei/Swiss mice model at 50 μmol/kg/day x 4. Pharmacomodulations should be further developed relying on a better knowledge on the porphyrin behaviour into the parasites comparatively to host cells. © 2013 Elsevier Masson SAS. All rights reserved.


Abada Z.,Alpha Chimica | Abada Z.,University Paris - Sud | Ferrie L.,University Paris - Sud | Akagah B.,Alpha Chimica | And 2 more authors.
Tetrahedron Letters | Year: 2011

General access to 5,15-diarylporphyrins in two steps is described. Generalization of this approach to tetra-substituted porphyrins allows the reproducible preparation of compounds, in some cases with high yields for porphyrins, which can be used in photodynamic therapy (PDT) in cancer today. © 2011 Published by Elsevier Ltd.


Abada Z.,Alpha Chimica | Abada Z.,University Paris - Sud | Ferrie L.,University Paris - Sud | Akagah B.,Alpha Chimica | And 2 more authors.
Tetrahedron Letters | Year: 2012

A first palladium catalyzed cross-coupling amination with chiral auxiliaries at the two meso positions of diarylporphyrins was reported. We noticed that, the non-metallation of porphyrins and steric hinderance of the chiral auxiliary play an essential role to the effectiveness of this cross coupling-reaction. Here, when two methyl pyroglutamates were added, the reaction leads to atropisomers and their behaviors were investigated by NMR spectroscopy. Finally, functionalizations of these chiral porphyrins were performed onto the pyrroglutamate moiety to give new original chiral porphyrins. © 2012 Elsevier Ltd. All rights reserved.

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