Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists

[摘要]：A structure-activity relationship study was undertaken to address the lack of oral exposure of the H3 antagonist 1, which incorporated an arylketone. Among a number of sub-series, the 4H-pyrido[1,2-a] pyrimidin-4-one analog 21 showed an improved PK profile in rat and mouse and was active in an obesity model. The pyrimidin-4-one proved to be a novel and useful ketone bioisostere. (C) 2012 Elsevier Ltd. All rights reserved.

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