Search Results - "Durieu, Véronique"
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1
Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol O‑Methyltransferase
Published in ACS medicinal chemistry letters (14-11-2019)“…A series of bicyclic pyridones were identified as potent inhibitors of catechol O-methyltransferase (COMT). Substituted benzyl groups attached to the basic…”
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2
Lead Optimization of Thiazolo[5,4-c]piperidines: 3-Cyclobutoxy Linker as a Key Spacer for H3R Inverse Agonists
Published in ChemMedChem (01-12-2012)“…The simpler, the better: H3 histamine receptor (H3R) are of interest as therapeutic targets in cognitive and somnolence disorders. Here, lead optimization of…”
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3
Acetamide Scanning around Bicyclic Thiazoles: SAR at the H 3 Receptor
Published in ChemMedChem (05-09-2011)Get full text
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4
Phenyl‐oxazoles, a New Family of Inverse Agonists at the H 3 Histamine Receptor
Published in ChemMedChem (01-02-2010)Get full text
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5
Discovery of a New Class of Non‐imidazole Oxazoline‐Based Histamine H 3 Receptor (H 3 R) Inverse Agonists
Published in ChemMedChem (06-07-2009)“…H 3 R inverse agonists based on an aminopropoxy‐phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse…”
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6
First dual M3 antagonists-PDE4 inhibitors : Synthesis and SAR of 4,6-diaminopyrimidine derivatives
Published in Bioorganic & medicinal chemistry letters (01-04-2006)“…SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M(3) antagonists and PDE4 inhibitors. Various chemical modulations…”
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7
Lead Optimization of Thiazolo[5,4‐ c ]piperidines: 3‐Cyclobutoxy Linker as a Key Spacer for H 3 R Inverse Agonists
Published in ChemMedChem (01-12-2012)Get full text
Journal Article -
8
Phenyl-oxazoles, a New Family of Inverse Agonists at the H3 Histamine Receptor
Published in ChemMedChem (01-02-2010)“…Drug design: Oxazoles and thiazoles were designed and synthesised based on previously reported ligands of the 3rd histamine receptor (H3R). The…”
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9
First dual M 3 antagonists-PDE4 inhibitors: Synthesis and SAR of 4,6-diaminopyrimidine derivatives
Published in Bioorganic & medicinal chemistry letters (01-04-2006)“…The synthesis and SAR around 4,6-diaminopyrimidine derivatives as dual M3 antagonists and PDE4 inhibitors are reported. SAR around 4,6-diaminopyrimidine…”
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10
Acetamide Scanning around Bicyclic Thiazoles: SAR at the H3 Receptor
Published in ChemMedChem (05-09-2011)“…A surprisingly homogeneous SAR against the H3 receptor was revealed for positional acetamide isomers of bicyclic thiazoles fused to various cyclic amines…”
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11
Lead optimization of thiazolo[5,4-c]piperidines: 3-cyclobutoxy linker as a key spacer for H(3)R inverse agonists
Published in ChemMedChem (01-12-2012)“…The simpler, the better: H(3) histamine receptor (H(3)R) are of interest as therapeutic targets in cognitive and somnolence disorders. Here, lead optimization…”
Get full text
Journal Article -
12
Discovery of a New Class of Non-imidazole Oxazoline-Based Histamine H3 Receptor (H3R) Inverse Agonists
Published in ChemMedChem (06-07-2009)“…H3R inverse agonists based on an aminopropoxy‐phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse…”
Get full text
Journal Article -
13
Phenyl-oxazoles, a new family of inverse agonists at the H(3) histamine receptor
Published in ChemMedChem (01-02-2010)Get full text
Journal Article -
14
Discovery of a new class of non-imidazole oxazoline-based histamine H(3) receptor (H(3)R) inverse agonists
Published in ChemMedChem (01-07-2009)“…H(3)R inverse agonists based on an aminopropoxy-phenyloxazoline framework constitute highly valuable druglike lead compounds that display efficacy in a mouse…”
Get full text
Journal Article -
15
First dual M sub(3) antagonists-PDE4 inhibitors: Synthesis and SAR of 4,6- diaminopyrimidine derivatives
Published in Bioorganic & medicinal chemistry letters (01-04-2006)“…SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M sub(3) antagonists and PDE4 inhibitors. Various chemical…”
Get full text
Journal Article