Many potential therapeutic properties have been recognized to carnosine (β-alanyl-l-histidine) but the therapeutic uses are strongly limited by its short lifetime in human plasma. This fact has been the main reason for developing the synthesis of various carnosine derivatives stable to carnosinase enzymes with interesting potentialities. Carnosine derivatives have been designed differently to conjugate the biological activity of carnosine with that of the functionalizing moiety. In the last years carnosine derivatives have been tested in vivo with very successful results, but until now there has been no application of these derivatives in vivo on human beings. These carnosine derivatives could represent the future drugs for many pathologies related to oxidative stress, reactive carbonyl species and metal-ion dyshomeostasis.