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

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Abstract

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. © 2012 Elsevier Ltd. All rights reserved.

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Xiao, D., Palani, A., Sofolarides, M., Aslanian, R., West, R. E., Williams, S. M., … Korfmacher, W. A. (2012). Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists. Bioorganic and Medicinal Chemistry Letters, 22(9), 3354–3357. https://doi.org/10.1016/j.bmcl.2012.02.076

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