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Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors. | LitMetric

Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors.

Bioorg Med Chem Lett

Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543-5400, USA.

Published: November 2010

AI Article Synopsis

  • - The study explores the creation and structure-activity relationship (SAR) of specific DPP4 inhibitors, focusing on aminomethyl-substituted imidazolopyrimidines with different aryl group attachments.
  • - Starting with Compound 1, which consists of non-interchangeable atropisomers, the research investigates how varying substituent patterns and types influence the effectiveness of the inhibitors.
  • - The findings highlight the importance of stereochemistry and the arrangement of substituents in determining the potency of these DPP4 inhibitors.

Article Abstract

The synthesis and SAR of aminomethyl-substituted imidazolopyrimidine DPP4 inhibitors bearing varied pendant aryl groups is described. Compound 1, which exists as a separable mixture of non-interconvertible atropisomers was used as the starting point for investigation. The effects of substituent pattern and type as well as stereochemical effects on inhibitor potency are discussed.

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Source
http://dx.doi.org/10.1016/j.bmcl.2010.08.090DOI Listing

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