OrganoCatalysed CannaBinoid Target-oriented synthesis of pyrazoline – OCat-CBtag

The increased demand from pharmaceutical industry for single-enantiomer heterocylic compounds, accessible by environmentally benign and economically reliable asymmetric catalytic methodologies, have placed the use of organocatalysts as major tools in that field. This project aims to construct a novel research group concerned by the achievement of organocatalytic biotarget-oriented stereoselective synthesis of libraries chiral pyrazoline derivatives, by means of the concept of masked hydrazine as building blocks. Our collaborative-program with biologists is driven by the rapid elaboration and evaluation of novel ligands for cannabinoid (CB) receptors based on pyrazoline scaffolds or congeners thereof. Such heterocycles are emerging as potent CB1 inverse agonist connected with extreme food intake and addiction problems (cigarette, drugs…). Obesity is recognized as a serious health concerns by the World Health Organization. Original dihydropyridine pyrazolines-derived prodrugs will be evaluated to deliver these ligands into the Central Nervous System through the lipophilic Blood Brain Barrier, based on Bodor's vectorisation concept. The selective modulation CB2 receptors in immune cells will be also studied to evolve into modulation of inflammations, allergies, etc, significant threat of the future.