Recherche de 5.

1. Modified 5'-trityl nucleosides as inhibitors of <em>Plasmodium falciparum</em> dUTPase (Publications)

   Modified 5'-trityl nucleosides as inhibitors of <em>Plasmodium falciparum</em> dUTPase

   Pertinence:

   discovery of 5'-tritylated analogues of deoxyuridine as selective inhibitors of this Plasmodium falciparum enzyme. Herein we report further structure-activity studies; in particular, variations of the 5'-trityl [...] ons of the base. Compounds were tested against both the enzyme and the parasite. Variations of the 5'-trityl group and of the 3'-substituent were well tolerated and yielded active compounds. However, there

2. Investigation of acyclic uridine amide and 5'-amido nucleoside analogues as potential inhibitors of the <em>Plasmodium falciparum</em> dUTPase (Publications)

   Investigation of acyclic uridine amide and 5'-amido nucleoside analogues as potential inhibitors of the <em>Plasmodium falciparum</em> dUTPase

   Pertinence:

   Previously we have shown that trityl and diphenyl deoxyuridine derivatives and their acyclic analogues can inhibit Plasmodium falciparum dUTPase (PfdUTPase). We report the synthesis of conformationall

3. Indian contribution to the cultural formulation interview and the DSM-5: missing details from the position paper [Letter to the editor] (Publications)

   Indian contribution to the cultural formulation interview and the DSM-5: missing details from the position paper [Letter to the editor]

   Pertinence:

4. 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential (Publications)

   3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential

   Pertinence:

   A novel class of orally active antimalarial 3,5-diaryl-2-aminopyridines has been identified from phenotypic whole cell high-throughput screening of a commercially available SoftFocus kinase library. The

5. 3-(oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid <em>Trypanosoma brucei</em>, the causative agent... (Publications)

   3-(oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid <em>Trypanosoma brucei</em>, the causative agent for human African trypanosomiasis

   Pertinence:

   investigation around one of these hit classes, the 3-(oxazolo[4,5-b]pyridin-2-yl)anilides. Sharp SAR is revealed, with our most active compound (5) exhibiting an IC50 of 91 nM against the human pathogenic strain

6. Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and... (Publications)

   Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres

   Pertinence:

   compared the antimalarial activities and ADME profiles of the 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres. Consistent with previous data, both dioxolanes had very weak antimalarial properties

7. Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, there prodrugs and aza-analogues (Publications)

   Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, there prodrugs and aza-analogues

   Pertinence:

   Fifty novel prodrugs and aza-analogues of 3,5-bis(4-amidinophenyl)isoxazole and its derivatives were prepared. Eighteen of the 24 aza-analogues exhibited IC50 values below 25nM against Trypanosoma brucei [...] for efficacy in mice infected with T. b. rhodesiense STIB900. Six diamidines cured 4/4 mice at daily 5mg/kg intraperitoneal doses for 4days, giving results far superior to pentamidine and furamidine. One

8. Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of... (Publications)

   Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity

   Pertinence:

   Replacement of the pyridine core of antimalarial 3,5-diaryl-2-aminopyridines led to the identification of a novel series of pyrazine analogues with potent oral antimalarial activity. However, other changes [...] core and replacement or substitution of the 2-amino group led to loss of antimalarial activity. The 3,5-diaryl-2-aminopyrazine series showed impressive in vitro antiplasmodial activity against the K1 (multidrug

9. Synthesis, crystal structure, and in vitro antiprotozoal activity of some 5-phenyl(methyl)sulfonyl-substituted dihydroisoxazoles (Publications)

   Synthesis, crystal structure, and in vitro antiprotozoal activity of some 5-phenyl(methyl)sulfonyl-substituted dihydroisoxazoles

   Pertinence:

10. Variabilité des maladies diarrhéiques chez les enfants de moins de 5 ans en milieu urbain: l'exemple de Rufisque au Sénégal (Publications)

    Variabilité des maladies diarrhéiques chez les enfants de moins de 5 ans en milieu urbain: l'exemple de Rufisque au Sénégal

    Pertinence: