A. Thomas

发表

Lead generation--enhancing the success of drug discovery by investing in the hit to lead process.

Alexander Alanine, A. Alanine, M. Nettekoven, 2003, Combinatorial chemistry & high throughput screening.

Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABA(A) alpha5 inverse agonist series.

F. Blasco, F. Knoflach, G. Trube, 2009, Bioorganic & medicinal chemistry letters.

Imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines as potent and highly selective GABAA alpha5 inverse agonists with potential for the treatment of cognitive dysfunction.

F. Knoflach, G. Trube, Maria-Clemencia Hernández, 2009, Bioorganic & medicinal chemistry letters.

Discovery of 4‐Substituted‐8‐(2‐hydroxy‐2‐phenyl‐cyclohexyl)‐2,8‐diaza‐spiro [4.5]decan‐1‐one as a Novel Class of Highly Selective GlyT1 Inhibitors with Improved Metabolic Stability.

E. Pinard, Daniel Zimmerli, D. Hainzl, 2006 .

Inhibition of alcohol self-administration by positive allosteric modulators of the GABAB receptor in rats: lack of tolerance and potentiation of baclofen

G. Gessa, P. Malherbe, F. Corelli, 2014, Psychopharmacology.

Pyrolysis Involving Compounds with CC, CN and CO Double Bonds

A. Thomas, R. Aitken, 2009 .

Modified mesoporous silicate MCM-41 materials: immobilised perruthenate—a new highly active heterogeneous oxidation catalyst for clean organic synthesis using molecular oxygen

A. Bleloch, S. Ley, A. Thomas, 1999 .

Modified Mesoporous Silicate MCM‐41 Materials: Immobilized Perruthenate — A New Highly Active Heterogeneous Oxidation Catalyst for Clean Organic Synthesis Using Molecular Oxygen.

A. Bleloch, S. Ley, A. Thomas, 2000 .

Organic synthesis provides opportunities to transform drug discovery

Anthony Wood, Andrew W. Thomas, David M. Wilson, 2018, Nature Chemistry.

Polymer-supported hypervalent iodine reagents in ‘clean’ organic synthesis with potential application in combinatorial chemistry

S. Ley, H. Finch, A. Thomas, 1999 .

Heterocyclic Acyl and Formyl Anion Equivalents

A. Thomas, R. Aitken, 2001 .

Synthesis of the alkaloids (±)-oxomaritidine and (±)-epimaritidine using an orchestrated multi-step sequence of polymer supported reagents

Steven V. Ley, S. Ley, A. Thomas, 1999 .

Clean synthesis of α-bromo ketones and their utilisation in the synthesis of 2-alkoxy-2,3-dihydro-2-aryl-1,4-benzodioxanes, 2-amino-4-aryl-1,3-thiazoles and piperidino-2-amino-1,3-thiazoles using polymer-supported reagents

S. Ley, James S. Scott, J. Scicinski, 1999 .

New vistas in quinoline synthesis

A. Thomas, R. Norcross, R. Masciadri, 2007 .

Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.

E. Pinard, J. Moreau, E. Borroni, 2008, Bioorganic & medicinal chemistry letters.

Expeditious solution phase synthesis of fluoroquinolone antibacterial agents using polymer supported reagents

A. Thomas, C. Hubschwerlen, Peter Hilty, 2001 .

A concise route to triazolobenzodiazepine derivatives via a one-pot alkyne-azide cycloaddition reaction.

A. Thomas, 2002, Bioorganic & medicinal chemistry letters.

Modern synthetic methods for copper-mediated C(aryl)[bond]O, C(aryl)[bond]N, and C(aryl)[bond]S bond formation.

S. Ley, A. Thomas, 2004, Angewandte Chemie.

Synthesis, structure and reactivity of some chiral benzylthio alcohols, 1,3-oxathiolanes and their S-oxides

P. Lightfoot, A. Thomas, R. Aitken, 2020 .

The positive allosteric modulator of the GABA(B) receptor, rac-BHFF, suppresses alcohol self-administration.

G. Gessa, P. Malherbe, P. Maccioni, 2010, Drug and alcohol dependence.

An improved synthesis of Lu AA20465

E. Pinard, A. Thomas, Eva A. Krafft, 2006 .

Reducing GABAA α5 Receptor-Mediated Inhibition Rescues Functional and Neuromorphological Deficits in a Mouse Model of Down Syndrome

M. Honer, R. Vidal, Á. Pazos, 2013, The Journal of Neuroscience.

Discovery of Small Molecule Therapeutics for Treatment of Chronic HBV Infection.

J. Young, Xingchun Han, Song Yang, 2018, ACS infectious diseases.

Characterization of (R,S)‐5,7‐di‐tert‐butyl‐3‐hydroxy‐3‐trifluoromethyl‐3H‐benzofuran‐2‐one as a positive allosteric modulator of GABAB receptors

W. Spooren, E. Prinssen, A. Sleight, 2008, British journal of pharmacology.

Positive Allosteric Modulation of GABAB Receptors Ameliorates Sensorimotor Gating in Rodent Models

P. Malherbe, R. Frau, M. Bortolato, 2014, CNS neuroscience & therapeutics.

Highly flexible and efficient synthesis of the GABAB enhancer 4-(2-hexylsulfanyl-6-methyl-pyrimidin-4-ylmethyl)-morpholine

P. Malherbe, E. Prinssen, A. Thomas, 2007 .

New Vistas in Quinoline Synthesis.

A. Thomas, R. Norcross, R. Masciadri, 2007 .

Efficient One-Pot Synthesis of the GABAB Positive Allosteric Modulator (R,S)-5,7-Di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one

P. Malherbe, A. Thomas, François Grillet, 2008 .

Efficient One‐Pot Synthesis of GABAB Positive Allosteric Modulator (R,S)‐5,7‐Di‐tert‐butyl‐3‐hydroxy‐3‐trifluoromethyl‐3H‐benzofuran‐2‐one.

P. Malherbe, A. Thomas, François Grillet, 2009 .

Reduction of alcohol intake by the positive allosteric modulator of the GABA(B) receptor, rac-BHFF, in alcohol-preferring rats.

G. Gessa, P. Malherbe, P. Maccioni, 2013, Alcohol.

Stereoselective synthesis of the cyclic ether core of (+)-laurenyne

Claire Wilson, S. Swallow, M. Cacho, 2004 .

Stereoselective Synthesis of the Cyclic Ether Core of (+)-Laurenyne.

Claire Wilson, S. Swallow, M. Cacho, 2005 .

RO4938581, a novel cognitive enhancer acting at GABAA α5 subunit-containing receptors

J. Moreau, F. Knoflach, G. Trube, 2008, Psychopharmacology.

Discovery of the Imidazo[1,5‐a][1,2,4]‐triazolo[1,5‐d][1,4]benzodiazepine Scaffold as a Novel, Potent and Selective GABAA α5 Inverse Agonist Series.

A. Thomas, 2010 .

Flash vacuum pyrolysis of oxazolidine-2,4-diones

A. Thomas, R. Aitken, 2002 .

Inhibition of alcohol self-administration by positive allosteric modulators of the GABAB receptor in rats: lack of tolerance and potentiation of baclofen

G. Gessa, P. Malherbe, F. Corelli, 2015, Psychopharmacology.

Basmisanil, a highly selective GABAA-α5 negative allosteric modulator: preclinical pharmacology and demonstration of functional target engagement in man

J. Hipp, L. Squassante, M. Honer, 2021, Scientific Reports.

A Straightforward and Efficiently Scaleable Synthesis of Novel Racemic 4-Substituted-2,8-diazaspiro[4.5]decan-1-one Derivatives

Daniel Zimmerli, A. Thomas, A. Kurt, 2005 .

The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.

F. Knoflach, G. Trube, H. Fischer, 2009, Bioorganic & medicinal chemistry letters.

Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.

E. Pinard, Daniel Zimmerli, D. Hainzl, 2006, Bioorganic & medicinal chemistry letters.

Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors.

S. Ceccarelli, E. Pinard, Daniel Zimmerli, 2006, Bioorganic & medicinal chemistry letters.

4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.

E. Pinard, Daniel Zimmerli, D. Hainzl, 2006, Bioorganic & medicinal chemistry letters.

Discovery of the imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepine scaffold as a novel, potent and selective GABA(A) alpha5 inverse agonist series.

F. Blasco, F. Knoflach, G. Trube, 2009, Bioorganic & Medicinal Chemistry Letters.

The positive allosteric modulator of the GABA(B) receptor, rac-BHFF, suppresses alcohol self-administration.

G. Gessa, P. Malherbe, P. Maccioni, 2010, Drug and alcohol dependence.