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1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.

Lübbers T, Böhringer M, Gobbi L, Hennig M, Hunziker D, Kuhn B, Löffler B, Mattei P, Narquizian R, Peters JU, Ruff Y, Wessel HP, Wyss P
Bioorg Med Chem Lett 17 2966-70 (2007)
Cited: 18 times
EuropePMC logo PMID: 17418568

Abstract

In a search for novel DPP-IV inhibitors, 2-aminobenzo[a]quinolizines were identified as submicromolar HTS hits. Due to the difficult synthetic access to this compound class, 1,3-disubstituted 4-aminopiperidines were used as model compounds for optimization. The developed synthetic methodology and the SAR could be transferred to the 2-aminobenzo[a]quinolizine series, leading to highly active DPP-IV inhibitors.

Articles - 2jid mentioned but not cited (3)

  1. The good, the bad and the dubious: VHELIBS, a validation helper for ligands and binding sites. Cereto-Massagué A, Ojeda MJ, Joosten RP, Valls C, Mulero M, Salvado MJ, Arola-Arnal A, Arola L, Garcia-Vallvé S, Pujadas G. J Cheminform 5 36 (2013)
  2. Identification of novel human dipeptidyl peptidase-IV inhibitors of natural origin (part I): virtual screening and activity assays. Guasch L, Ojeda MJ, González-Abuín N, Sala E, Cereto-Massagué A, Mulero M, Valls C, Pinent M, Ardévol A, Garcia-Vallvé S, Pujadas G. PLoS One 7 e44971 (2012)
  3. Design, Synthesis and Biological Evaluation of N4-Sulfonamido-Succinamic, Phthalamic, Acrylic and Benzoyl Acetic Acid Derivatives as Potential DPP IV Inhibitors. Khalaf RA, Sheikha GA, Al-Sha'er M, Taha M. Open Med Chem J 7 39-48 (2013)


Reviews citing this publication (4)

  1. Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes. Havale SH, Pal M. Bioorg Med Chem 17 1783-1802 (2009)
  2. Recent approaches to medicinal chemistry and therapeutic potential of dipeptidyl peptidase-4 (DPP-4) inhibitors. Patel BD, Ghate MD. Eur J Med Chem 74 574-605 (2014)
  3. Recent patents of dipeptidyl peptidase IV inhibitors. Mendieta L, Tarrago T, Giralt E. Expert Opin Ther Pat 21 1693-1741 (2011)
  4. Activity and selectivity cliffs for DPP-IV inhibitors: Lessons we can learn from SAR studies and their application to virtual screening. Ojeda-Montes MJ, Gimeno A, Tomas-Hernández S, Cereto-Massagué A, Beltrán-Debón R, Valls C, Mulero M, Pujadas G, Garcia-Vallvé S. Med Res Rev 38 1874-1915 (2018)

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