Synthèse, caractérisation et évaluation biologique De nouveaux dérivés hétérocycliques

Abstract

In this manuscript, subdivided into three chapters, we are interested in the development of simple and effective new approaches for the synthesis of new functional and structural diversified heterocyclic and poly-heterocyclic systems, which represent potential biological activities. In the first chapter, we proceeded to the synthesis of the new [1,8] -naphthyridines derivatives and their tetracyclic analogs by the development of an efficient multi-step synthesis strategy. AChE and BuChE inhibition potency of synthesized products was evaluated in vitro as well as their antioxidant power. Analysis of obtained results as well as an additional study carried out by Molecular Doking confirmed the effectiveness of these molecules, specially compound 4, as multi-target agents for the treatment of AD. In the second chapter, we focused on the synthesis of new Zoledronate analogs, with a variously substituted triazole motif, via click chemistry reactions. These new gembisphosphonate derivatives was synthesized for the purpose of designing compounds with high FPPS inhibiting potency, as well as good passive penetration through the cancer cell’s membrane. The last chapter was devoted to an exclusive study comparing the catalytic efficiency of a series of different synthesized pyridinium, phosphonium or imidazolium based ionic liquids, in the synthesis of a varied range of 4H-pyran derivatives by one pot Biginelli-like multi component reaction.