Development of compounds acting on CNS

Three main research lines: i) cholinesterases inhibition, ii) BACE-1 inhibition, iii) development of diagnostics.

i) Potent human cholinesterase reversible inhibitors as potential drugs for the treatment of Alzheimer’s disease have been developed; the developed ligands allowed the targeting of key enzyme hot-spots at the active site gorge level of cholinesterases; ii) A series of benzodiazepine-based BACE-1 peptidomimetic inhibitors and their seco-analogues have been developed as druggable scaffolds for obtaining potential anti-Alzheimer’s disease therapeutics; iii) Compounds specifically targeting amyloid plaques as potential diagnostic tools for Alzheimer’s disease have been developed.

Researchers involved

• Giuseppe Campiani

Three main research lines: i) development of atypical antipsychotics ii) D3 selective ligands, iii) 5-HT3 ligands.

i) This research activity allowed the proposal and validation of an innovative multireceptor affinity profile for developing a new class of potent atypical antipsychotics in vivo (animal models); ii) Potent and selective D3 receptor ligands, endowed with different intrinsic efficacy, for the treatment of Drug-seeking behavior have been developed; iii) A huge number of potent and selective serotonin 5-HT3 agonist have been identified. The rational modification of these compounds allowed the obtainment of either brain penetrating or peripheral agents (unable to cross the Blood Brain Barrier).

Researchers involved

• Giuseppe Campiani