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Dive into the research topics where Etzer Darout is active.

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Featured researches published by Etzer Darout.


Journal of Medicinal Chemistry | 2011

Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.

Kim F. McClure; Etzer Darout; Cristiano R. W. Guimarães; Michael Paul Deninno; Vincent Mascitti; Michael John Munchhof; Ralph P. Robinson; Jeffrey T. Kohrt; Anthony R. Harris; Dianna E. Moore; Bryan Li; Lacey Samp; Bruce Allen Lefker; Kentaro Futatsugi; Daniel Kung; Paul D. Bonin; Peter Cornelius; Ruduan Wang; Eben Salter; Sam Hornby; Amit S. Kalgutkar; Yue Chen

The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agonist pharmacology are used to formulate a conformation-based hypothesis to understand activation of the GPR119 receptor. We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology.


Archive | 2010

Gpr 119 modulators

Etzer Darout; Cristiano R. W. Guimarães; Vincent Mascitti; Kim F. McClure


Archive | 2015

SUBSTITUTED AMIDE COMPOUNDS

Etzer Darout; Kim F. McClure; David W. Piotrowski; Brian Raymer


Tetrahedron Letters | 2010

The synthesis of azabicyclic heterocycles

Etzer Darout; Arindrajit Basak


Tetrahedron Letters | 2011

Synthesis of two novel regioisomeric oxospiropyrazole piperidine scaffolds

Benjamin D. Stevens; Etzer Darout; Vincent Mascitti; Kim F. McClure


Synthesis | 2013

Study of the Kulinkovich Synthesis of 1-Methylcyclopropanol and Its Conversion into 1-Methylcyclopropyl 4-Nitrophenyl Carbonate

Stephen W. Wright; Etzer Darout; Benjamin D. Stevens


Phosphodiesterases and Their Inhibitors | 2014

PDE4: Recent Medicinal Chemistry Strategies to Mitigate Adverse Effects

Etzer Darout; Elnaz Menhaji-Klotz; Thomas A. Chappie


Archive | 2014

N-PIPERIDIN-3-YLBENZAMIDE DERIVATIVES FOR TREATING CARDIOVASCULAR DISEASES

Etzer Darout; Robert Dullea; Julie Hawkins; Allyn T. Londregan; Paula M. Loria; Bruce Maguire; Kim F. McClure; Donna N. Petersen; David W. Piotrowski


Tetrahedron | 2012

Synthesis of spirofuranopyrimidine–piperidines

Etzer Darout; Kim F. McClure; Vincent Mascitti


Archive | 2015

Composés d'amide substitué

Etzer Darout; Kim F. McClure; David W. Piotrowski; Brian Kenneth Raymer

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