Screening strategy for chiral and achiral separations in supercritical fluid chromatography mode.

Supercritical fluid (SF) was discovered 200 years ago, but the use of this fluid as a mobile phase in chromatography only became popular fifty years ago. The development of the supercritical fluid chromatography (SFC) was progressing slowly due to technological problems since ten years; the interest for this chromatographic mode has been growing up as the construction of the SFC instruments is more or less similar with HPLC instruments. The main difference in SFC is the installation of a back pressure regulator which is implemented to control the pressure above the critical pressure.

Conformational analysis of r207910, a new drug candidate for the treatment of tuberculosis, by a combined NMR and molecular modeling approach.

R207910 is an enantiomeric compound from a new class of antimycobacterial agents, the diarylquinolines [Science; 307:223 (2005)]. As enantiospecific interaction is required for biologic activity, we have undertaken a combined nuclear magnetic resonance and molecular modeling study to gain new insights into its conformation in solution and its absolute configuration. A conformational analysis using a Monte-Carlo method has been performed on each of the four possible stereomers of this compound leading to the identification of their most stable conformation.

Discovery of pyrimidyl-5-hydroxamic acids as new potent histone deacetylase inhibitors.

A series of pyrimidyl-5-hydroxamic acids was prepared for evaluation as inhibitors of histone deacetylase (HDAC). Amino-2-pyrimidinyl can be used as a linker to provide HDAC inhibitors of good enzymatic potency.