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

  • Xiao D
  • Palani A
  • Sofolarides M
 et al. 
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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.

Author-supplied keywords

  • H3 antagonists
  • Ketone bioisostere

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  • Dong Xiao

  • Anandan Palani

  • Michael Sofolarides

  • Robert Aslanian

  • Robert E. West

  • Shirley M. Williams

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