Synthesis and Biological Activity of N-substituted Carnosine Amide Derivatives

A series of carnosine derivatives were synthesized by modification of primary amino groups of carnosine, eleven target compounds were obtained and characterized by NMR, UV-Vis and HR-MS. Acrolein scavenging activity test results showed that most compounds exhibited some acrolein scavenging activities, especially compound 4k showed the highest acrolein scavenging activity which was stronger than carnosine. Spleen cell proliferation test results showed that most compounds exhibited some spleen cell proliferation activities, compounds 4b, 4d and 4k showed stronger spleen cell proliferation activities than the positive control conA. Hydrogen peroxide injury pre-protection results showed that most compounds exhibited some pre-protection effects, especially compounds 4a, 4j and 4k showed stronger ECV-304 cell pre-protection effects than carnosine. Plasma stability assay results showed that compared with carnosine, eleven compounds had good plasma stability.