Design,synthesis and preliminary anti-radiation activityof novel LPA2 receptor agonists / 国际药学研究杂志

Objective To design and synthesize novel G protein-coupled lysophosphatidic acid 2(LPA2)receptor agonists with anti-radiation activity. Methods Nine new LPA2 receptor agonists(Ⅰ2-Ⅰ5 andⅡ1-Ⅱ5)were designed and synthesized using DBIBB as the lead compound. The anti-radiation activity was assayed by the MTS method using the human umbilical vein endothelial cells(HUVEC)irradiated with 8.0 Gy 60Coγray. Results and Conclusion Nine target compounds notreported in the literature were synthesized and their structures were confirmed by 1H NMR and MS. The results showed thatⅠ4 andⅡ1 have obvious anti-radiation ac-tivity,indicating that this kind of compounds is worth further studying.