Projects

Digestive Lipases Inhibitors

Lipids constitute a large part of the biomass of living organisms, and lipolytic enzymes play an essential role in the turnover of this material. In particular, triglycerides (triacylglycerols, TAGs) constitute the major part (95%) of dietary lipids. Human pancreatic (HPL) and gastric (HGL) lipases are essential enzymes for efficient fat digestion. The hydrolysis of dietary TAGs by these enzymes to monoacylglycerols and free fatty acids is a necessary step for fat absorption by the enterocytes.

Inhibitors of the Enzymes of the Endocannabinoid System

Cannabis sativa is one of the oldest plants cultivated by the human race, not for food, but for its use for medical and recreational purposes.  The Chinese seem to have used it both as medicine and as textile for its fibers as early as in 4000 B.C. In India, the medical and religious use of Cannabis begun around 1000 B.C., while Herodotus described a Scythian funeral ceremony in 450 B.C. where cannabis seeds burned and the participants inhaled its vapors as part of the ritual.

NHCs as Organocatalysts

Hydroxymethyl ketones are useful auxiliaries in organic synthesis and are also found in several medicinal agents. N-Heterocyclic carbenes (NHCs) have been used in the literature in order to introduce the hydroxymethyl group into aromatic aldehydes in good yields, but they are not that successful for aliphatic aldehydes. We present the use of microwave irradiation that has been efficiently incorporated into an organocatalytic synthesis of aromatic, but more importantly of aliphatic hydroxymethyl ketones that can be used as precursors for medicinally interesting compounds.

Phospholipase A2 Inhibitors - iPLA2 Inhibitors

The phospholipase A2 (PLA2) superfamily consists of many different groups of enzymes that catalyze the hydrolysis of the ester bond at the sn-2 position of various phospholipids. The products of the hydrolysis are a free fatty acid and a lysophospholipid, which both may generate second messengers that play important physiological roles. The PLA2 superfamily currently contains 15 separate, identifiable groups and various subgroups.