Synthesis and biological evaluation of new potential co-adjuvants for the treatment of Parkinson’s disease and a new catalytic, asymmetric approach to the synthesis of fused heterocycles of biological interest.

Medicinal chemistry and pure organic chemistry were merged in this thesis as two faces of the same coin. In the first part, more than a hundred hydrazothiazole derivatives were synthesized and tested as human monoamine oxidase B selective inhibitors in order to define accurate structure activity relationships. Our knowledge on human MAO-B inhibition was then applied to the synthesis of purine derivatives as potential dual human MAO-B inhibitors and adenosine A2A receptor antagonists. In the second part, the search for a new catalytic, asymmetric route to the synthesis of poly(hetero)cyclic compounds of biological interest led to the development of a new enantioselective approach to the phase transfer catalyzed cyclization of pyrrole derived substrates.