Synthesis And Photoprotection Research Of Aryl Thiazole Derivatives

Solar irradiation is including three main spectrums that are ultraviolet range (400nm-100nm,7%), visible light (780nm-400nm,50%) and infrared range (106nm-780nm,53%). Excessive exposure to ultraviolet radiation (UV) is believed to induce various skin diseases such as sunburn, photo-aging and photo-immunosuppression. Moreover, skin oncology research has proved acute or chronic UV exposure is responsible for photocarcinogenesis as one of the key factors in the process of skin cancer. As a direct and effective method for photo-protection, commercial sunscreens have been used since1928as the most prevalent protection strategy and which has still played a major role in photo-protection and skin cancer prevention until today. Among UV light, UVB (280-320nm) is a predominate and most harmful component, which was regarded as main reason for the most severe damageA series of new aryl thiazole derivatives in preventing keratinocyte cell (HaCaT) from UVB-induced cellar damage have been designed, synthesized and evaluated. The structure-activity relationship was discussed from chemical modification of amide, aryl-thiazole rings and the linker. Preliminary data suggested that compound5a,11a,13c and17can protect more effectively Keratinocytes cell from UVB-induced cell death than positive control polydatin in vitro. Extensive structure exploration and activity assay lead to the selection of compound5a for following in vivo studies and the result demonstrated that compound5a significantly protected the dorsal skin of BALB/c-nu mice against UVB-induced decrustation. Our studies indicated that these aryl thiazole derivatives, especially compound5a, can be considered as a novel potential photo-protection agent or a promising sunscreen candidate.