Synthesis of small molecule-peptide conjugates as potential whitening agents

Authors: Lee, Hye-Suk; Shin, Kyong-Hoon; Ryu, Geun-Seok; Chi, Gyeong-Yup; Cho, In-Shik; Kim, Han-Young; Bulletin of the Korean Chemical Society; (2012); 10.5012/bkcs.2012.33.9.3004

Small molecule conjugated peptides were prepared by solid-phase synthesis as potential novel whitening agents, and their melanogenesis inhibitory activities were investigated. The conjugated small molecules were well-known materials as tyrosinase inhibitors, and peptides were selected from the sequences that are known to antagonize melanocortin receptor 1 (MC1R). Most of small molecules-peptide conjugates showed superior melanin inhibition activity to kojic acid and arbutin. Among these, almost all compounds have -AR- sequence. From this study, we concluded that the small molecule conjugated peptides containing -AR- sequence have melanogenesis inhibitory activities and have potential to be used as novel whitening agents.