Here, a new class of benzylpiperidine-basedMAGL inhibitors was synthesized, leading to the identification of 13, which showed potent reversible and selective MAGL inhibition.Associated with MAGL overexpression and the prognostic role in pancreaticcancer, derivative 13 showed antiproliferative activityand apoptosis induction, as well as the ability to reduce cell migrationin primary pancreatic cancer cultures, and displayed a synergisticinteraction with the chemotherapeutic drug gemcitabine. The gene discussed is MGLL; the disease is pancreatic neoplasm.