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Antimalarial potential of xestoquinone, a protein kinase inhibitor isolated from a Vanuatu marine sponge Xestospongia sp.
- D. Laurent, V. Jullian, +11 authors M. Sauvain
- Chemistry, Medicine
- Bioorganic & medicinal chemistry
- 1 July 2006
Xestoquinone exhibited a weak in vivo activity in Plasmodium berghei NK65 infected mice and was toxic at higher doses, and in vitro antiplasmodial activity against a FCB1 P. falciparum strain with an IC(50) of 3 microM and a weak selectivity index (SI 7). Expand
Antiplasmodial Activities of Homogentisic Acid Derivative Protein Kinase Inhibitors Isolated from a Vanuatu Marine Sponge Pseudoceratina sp.
A bioassay-guided fractionation led to the isolation of a derivative of homogentisic acid [methyl (2,4-dibromo-3,6-dihydroxyphenyl)acetate, 4a] which inhibited Pfnek-1 with an IC50 around 1.8 μM. Expand
Acaricidal activity of essential oils from five endemic conifers of New Caledonia on the cattle tick Rhipicephalus (Boophilus) microplus
- N. Lebouvier, T. Hue, E. Hnawia, Leïla Lesaffre, C. Menut, M. Nour
- Biology, Medicine
- Parasitology Research
- 31 January 2013
This study shows that A. columnaris and N. pancheri could provide valuable and effective natural acaricides for control of the cattle tick R. microplus. Expand
Structure-activity relationship study of biflavonoids on the Dengue virus polymerase DENV-NS5 RdRp.
Over the four different biflavonoid skeletons tested, amentoflavone and robustaflavone are the most promising ones for antidengue drug development, and Sotetsuflavone is the most active compound of this series and is the strongest inhibitor of the Dengue virus NS5 RNA-dependent RNA polymerase described in the literature. Expand
Biflavonoids of Dacrydium balansae with potent inhibitory activity on dengue 2 NS5 polymerase.
P podocarpusflavone A is the strongest noncytotoxic non-nucleotide molecule exhibiting a specific inhibitory activity against the RNA polymerase domain of DV-NS5 and thus is promising for chemotherapy development against dengue fever. Expand
The Wound Healing and Antibacterial Activity of Five Ethnomedical Calophyllum inophyllum Oils: An Alternative Therapeutic Strategy to Treat Infected Wounds
The cytotoxic, wound healing, and antibacterial properties of five CIO traditionally used to treat infected wounds were evaluated and the pharmacological effects of CIO as wound healing and antimicrobial agent were confirmed. Expand
New Inhibitors of the DENV-NS 5 RdRp from Carpolepis laurifolia as Potential Antiviral Drugs for Dengue Treatment
Since a few decades the dengue virus became a major public health concern and no treatment is available yet. In order to propose potential antide ngue compounds for chemotherapy we focused on DENV R… Expand
Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety.
- N. Lebouvier, F. Pagniez, +4 authors M. Le Borgne
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 1 July 2007
A series of fluconazole analogues 5-20 incorporating azaindole and indole moieties were prepared using oxirane intermediates synthesized under microwave irradiation and exerted high antifungal activity against C. albicans and Aspergillus fumigatus in vitro. Expand
Efficient microwave-assisted synthesis of 1-(1H-indol-1-yl)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents
New conazole antifungals, in the series of triazole alcohols 23a–d and 24a–e incorporating an indole moiety substituted at 5-position by halogens, a cyano or 4-methoxyphenyl group, have been… Expand
Lewis acid activation of chiral 2-trifluoromethyl-1,3-oxazolidines. Application to the stereoselective synthesis of trifluoromethylated amines, α- and β-amino acids
The reaction of chiral 2-trifluoromethyl-1,3-oxazolidines with various silylated nucleophiles under Lewis acid activation provides a stereoselective route to functionalized α-trifluoromethylamines.… Expand