Exposure to radiation through a nuclear accident or explosion of a �dirty bomb,� is now a major public health threat. To date, there are no FDA approved radiomitigators available for the recovery of immune, hematopoietic and gastrointestinal compartments following radiation injury. Radiomitigators also provide potential therapeutic applications in the attenuation of the side effects of radiation therapy and chemotherapy like diarrhea in cancer patients. In an effort to discover novel highly potent radiomitigators, we designed and synthesized sulfamoyl benzoic acid (SBA) analogs as the first non-lipid specific agonists of the type 2 GPCR for lysophosphatidic acid (LPA2). Our research group identified a picomolar agent 5-chloro-2-(N-(4-(1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)butyl)sulfamoyl)benzoic acid (RP-10-83  ; EC50 (nM): 5.06x10-3�3.73x10-3) as specific non-lipid LPA2 receptor agonist.

Design and synthesis of novel sulfamoyl benzoic acid (SBA) analogs as specific non-lipid LPA2 receptor agonists with picomolar affinities

248th National Meeting (2014)

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