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The coagulation enzyme factor Xa (FXa) is a valuable target for developing anticoagulants to treat thrombotic diseases. In this work, we designed and synthesized a series of conformationally restricted compounds containing the benzo[1,3]oxazinyloxazolidinone scaffold. The target compounds were synthesized by 11 steps reaction. The preliminary SAR showed that on the phenyl ring of benzo[1,3]oxazinyloxazolidinone, lactam replacements at the 6-position were favorable for FXa inhibition. Compound  16b  showed good FXa inhibitory activity with an IC 50  of 0.43 μM. The results indicate that benzo[1,3]oxazinyloxazolidinone is a promising scaffold for developing FXa inhibitors as antithrombotic agents.

Design and synthesis of tricyclic benzo[1, 3]oxazinyloxazolidinones as blood coagulation factor Xa inhibitors