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Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and
In vivo phosphorylation of FTY720 (1) in rats and humans resulted exclusively in the biologically active (S)-configured enantiomer, which was proven by an ex vivo o-phthaldialdehyde derivatizationExpand
Enantioselective chromatography as a powerful alternative for the preparation of drug enantiomers.
  • E. Francotte
  • Chemistry, Medicine
  • Journal of chromatography. A
  • 12 January 2001
The possible contribution of enantioselective chromatography with respect to the preparation ofEnantiomerically pure compounds is reviewed in the context of the competitive approaches and depending on the application scale, with a special emphasis on the recent progresses achieved in this particular field of separation. Expand
Chiral inversion and hydrolysis of thalidomide: mechanisms and catalysis by bases and serum albumin, and chiral stability of teratogenic metabolites.
1H NMR experiments revealed that the three teratogenic metabolites of thalidomide, in sharp contrast to the drug itself, had complete chiral stability, which leads to the speculation that, were some enantioselectivity to exist in the teratogenicity ofThalidomid, it could result from fast hydrolysis to chirally stable ter atogenic metabolites. Expand
Chiral resolution, pharmacological characterization, and receptor docking of the noncompetitive mGlu1 receptor antagonist (+/-)-2-hydroxyimino- 1a,
A molecular mechanics model of the putative seven TM domain of hmGlu1 based on the alpha-carbon template of the TM helices of rhodopsin is built to suggest a plausible binding mode of (-)-1. Expand
Spirotetrahydro β-Carbolines (Spiroindolones): A New Class of Potent and Orally Efficacious Compounds for the Treatment of Malaria
Improvement of the pharmacokinetic profile of the series translated to exceptional oral efficacy in the P. berghei infected malaria mouse model where full cure was achieved in four of five mice with three daily doses of 30 mg/kg. Expand
Supercritical fluid chromatography in pharmaceutical analysis.
In the present review, the instrumentation and experimental conditions to perform "advanced SFC" are discussed and the applicability of SFC in pharmaceutical analysis, including the determination of drugs in formulations and biofluids is critically discussed. Expand
Benzoyl cellulose beads in the pure polymeric form as a new powerful sorbent for the chromatographic resolution of racemates
Cellulose-based stationary phases are known to be very efficient and versatile chiral sorbents for the chromatographic resolution of racemates. Except for microcrystalline cellulose triacetate (CTAExpand
Chromatographic resolution on methylbenzoylcellulose beads: Modulation of the chiral recognition by variation of the position of the methyl group on the aromatic ring
Abstract The preparation of cellulose-based chiral stationary phases (CSPs) in the pure polymer from (i.e., without an achiral support such as silica gel), according to a process already reported forExpand
Applications of simulated moving-bed chromatography to the separation of the enantiomers of chiral drugs
Although most preparative chiral separations have been performed in the conventional batch-mode process, interest in simulated moving-bed (SMB) chromatography is growing, because it permits largeExpand