[Research progress of liver X receptor agonists].

Liver X receptor (LXR), a member of the superfamily of nuclear receptors, plays an important role in the activation of transcription factors involved in cholesterol metabolism, glucose homeostasis inflammation and lipogenesis. It is shown that LXR agnoists have the potentiality to be used as drugs for the prevention and treatment of atherosclerosis, which is its best investigated therapeutic indication. There are many compounds being studied in preclinical evaluation and biological assay. This paper will review briefly the LXR agonists in recent years.

(Z)-3',6'-Bis(diethyl-amino)-2-(4-oxopent-2-en-2-yl-amino)-spiro-[isoindoline-1,9'-xanthen]-3-one.

In the title compound, C(33)H(38)N(4)O(3), the mean planes of the 9H-xanthene unit and spiro-lactam (nine-atom) core are almost mutually perpendicular at 87.26 (6)°. Intra-molecular N-H⋯O and C-H⋯N inter-actions influence the 4-oxo-pent-2-en-2-yl-amino conformation. In the crystal, weak C-H⋯O hydrogen bonds link the mol-ecules into chains along [001].

2-(4-Fluoro-phen-yl)-4-(4-meth-oxy-phen-yl)-5-(piperidin-1-ylmeth-yl)thia-zole.

In the title compound, C(22)H(23)FN(2)OS, the piperidine ring shows chair confirmation and the two benzene rings make a dihedral angle of 17.0 (6)°. The thia-zole fragment is essentially planar with an r.m.s. deviation of 0.004 (2) Šand a maximum deviation of 0.006 (2) Å.. In the crystal, inter-molecular C-H⋯π inter-actions lead to the formation of a layer structure.

[Advances in the study of anti-atherosclerosis drugs].

Several new drug targets of anti-atherosclerosis, emerging in the recent years, such as PPAR agonists, cholesteryl ester transfer protein (CETP) inhibitors, infusion of apolipoprotein A-I (apoA-I), liver X receptor (LXR) activators and phospholipid transfer protein (PLTP) inhibitors etc were reviewed.