Zobrazeno 1 - 10
of 41
pro vyhledávání: '"Michèle Calas"'
Autor:
Michel Boisbrun, Henri Vial, Suzanne Peyrottes, Karine Alarcon, Michèle Calas, Xavier J. Salom-Roig, Marjorie Maynadier, Mahama Ouattara, Sergio A. Caldarelli, Sharon Wein, Alain Pellet, Abdallah Hamze
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3953-3956
We report here the synthesis and biological evaluation of a series of 37 compounds as precursors of potent antimalarial bis-thiazolium salts (T3 and T4). These prodrugs were either thioester, thiocarbonate or thiocarbamate type and were synthesized i
Autor:
Michèle Calas, Henri Vial, Françoise Bressolle, Olivier Nicolas, Nicolas Taudon, Delphine Margout
Publikováno v:
Journal of Chromatography B. 820:83-93
Liquid chromatography-electrospray ionization mass spectrometry methods are described for the simultaneous quantification of a bis-thiazolium compound (T3), its related prodrug (TE3) and an intermediate compound (mTE3) that appeared during the prodru
Publikováno v:
Clinical Chemistry. 51:593-602
Background: A new class of antimalarial drugs targeting membrane biogenesis during intraerythrocytic Plasmodium falciparum development has been identified. The bisthiazolium salts T3 and T4 have superior in vitro and in vivo parasite-killing properti
Autor:
Olivier Nicolas, Michèle Calas, Henri Vial, Marie-Laure Ancelin, Françoise Bressolle, Sharon Wein, Clemens H. M. Kocken, Alan W. Thomas, Christine Farenc
Publikováno v:
Proceedings of the National Academy of Sciences. 101:15458-15463
We created neutral antimalarial prodrugs that deliver bisthiazolium compounds with antimalarial activity in the nanomolar range. These drugs primarily affect early intraerythrocytic stages through rapid, nonreversible cytotoxicity. The compounds are
Publikováno v:
Antimicrobial Agents and Chemotherapy. 47:2598-2605
We previously showed that quaternary ammonium salts have potent antimalarial activities against the blood stage of drug-resistant Plasmodium falciparum . In the present study, 13 compounds of this series were comparatively assessed in murine in vivo
Autor:
Valérie Vidal-Sailhan, Michèle Calas, Marie L. Ancelin, Pascal Ringwald, Serge Herbute, Henri Vial
Publikováno v:
Antimicrobial Agents and Chemotherapy. 47:2590-2597
We characterized the potent in vitro antimalarial activity and biologic assessment of 13 phospholipid polar head analogs on a comparative basis. There was a positive relationship between the abilities of the drugs to inhibit parasite growth in cultur
Autor:
Musa Z. Nazer, Michèle Calas, Shadia F. Okasha, Jacques Bompart, Mustafa M. El-Abadelah, Pierre Mion
Publikováno v:
European Journal of Medicinal Chemistry. 33:33-42
A series of 7-aryl-4-oxothieno[2,3- b ]pyridine-5-carboxylic acids 8 and their methyl esters 7 were synthesized by intramolecular cyclization of the respective 3- N -arylamino-2-(2,5-dichloro-3-thenoyl) acrylates 6 . The latter are accessible from me
Autor:
Henri Vial, Jacques Bompart, Michèle Calas, Gérard Cordina, Ben Bari M, Marie-Laure Ancelin, Jei T
Publikováno v:
Journal of Medicinal Chemistry. 40:3557-3566
A series of 80 compounds, primary, secondary, and tertiary amines and quaternary ammonium and bisammonium salts, most of them synthesized as potential choline or ethanolamine analogs, were tested against the in vitro growth of Plasmodium falciparum,
Autor:
Henri Vial, Alan W. Thomas, Chris J. Janse, J. Bourguignon, Michèle Calas, Christian Slomianny, Pascal Ringwald, Sócrates Herrera, Marie-Laure Ancelin, F. Louis, Louis Giral, Wallace Peters
Publikováno v:
Annals of Tropical Medicine & Parasitology. 91:S87-S90
A programme for developing new drugs for the treatment of Plasmodium falciparum malaria is targeted against the essential phospholipid metabolism of the intra-erythrocytic stages of the parasite. Blockage of the choline transporter that provides the
Autor:
Sharon Wein, Henri Vial, Michèle Calas, Alan W. Thomas, Sócrates Herrera, Françoise Bressolle
Publikováno v:
médecine/sciences. 21:341-343
> Le paludisme constitue la premiere endemie parasitaire dans le monde. Pres de 40% de la population mondiale vit en zone a risque et on enregistre entre 300 et 500 millions de cas cliniques chaque annee avec plus de unmillion de deces, principalemen