Literature DB >> 20833042

Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors.

Stephen P O'Connor1, Ying Wang, Ligaya M Simpkins, Robert P Brigance, Wei Meng, Aiying Wang, Mark S Kirby, Carolyn A Weigelt, Lawrence G Hamann.   

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.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20833042     DOI: 10.1016/j.bmcl.2010.08.090

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Predictive Model for Site-Selective Aryl and Heteroaryl C-H Functionalization via Organic Photoredox Catalysis.

Authors:  Kaila A Margrey; Joshua B McManus; Simone Bonazzi; Frederic Zecri; David A Nicewicz
Journal:  J Am Chem Soc       Date:  2017-08-07       Impact factor: 15.419

Review 2.  Atropisomerism in medicinal chemistry: challenges and opportunities.

Authors:  Sean T Toenjes; Jeffrey L Gustafson
Journal:  Future Med Chem       Date:  2018-01-30       Impact factor: 3.808

  2 in total

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