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Drug Discovery Today, ISSN 1359-6446, 10/2017, Volume 22, Issue 10, pp. 1478 - 1488
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2015, Volume 58, Issue 20, pp. 8216 - 8235
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 03/2019, Volume 62, Issue 6, pp. 2974 - 2987
In Alzheimer's disease, the density and spread of aggregated tau protein track well with neurodegeneration and cognitive decline, making the imaging of... 
AGENT | NEUROFIBRILLARY TANGLES | F-18-AV-1451 | CHEMISTRY, MEDICINAL | ALZHEIMERS-DISEASE | PET
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 06/2018, Volume 61, Issue 12, pp. 5292 - 5303
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 03/2015, Volume 6, Issue 3, pp. 282 - 286
A novel series of pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines is reported as potent PDE2/PDE10 inhibitors with drug-like properties. Selectivity for PDE2 was... 
phosphodiesterase 2 inhibitor | Pyrido[4 3- e ]triazolo[4 3- a ]pyrazine | selective | tricycle | PDE2 inhibitor | POTENT | CHEMISTRY, MEDICINAL | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES | Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazine | DISCOVERY
Journal Article
ACS MEDICINAL CHEMISTRY LETTERS, ISSN 1948-5875, 08/2019, Volume 10, Issue 8, pp. 1159 - 1165
Despite several years of research, only a handful of beta-secretase (BACE) 1 inhibitors have entered clinical trials as potential therapeutics against... 
CLEAVING ENZYME | DESIGN | HIT | CHEMISTRY, MEDICINAL | cyclic sulfamidates | ALZHEIMERS-DISEASE | pK(a) | BACE inhibitor | beta-secretase 1 | Alzheimer's disease | BACE1 INHIBITORS
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 09/2014, Volume 5, Issue 9, pp. 1049 - 1053
Structure-guided design led to the identification of the novel, potent, and selective phosphodiesterase 2 (PDE2) inhibitor 12. Compound 12 demonstrated a... 
phosphodiesterase 2 | target engagement | PDE2 inhibitor | [1,2,4]triazolo[4,3- a ]quinoxalines | CHEMISTRY, MEDICINAL | SERIES | PERFORMANCE | OBJECT MEMORY | LTP | DISCOVERY | HIPPOCAMPUS | CONSOLIDATION | [1,2,4]triazole[4,3-a]quinoxalines | CGMP | PHOSPHODIESTERASES | CAMP
Journal Article
European Journal of Organic Chemistry, ISSN 1434-193X, 12/2012, Volume 2012, Issue 36, pp. 7048 - 7052
A simple and scalable procedure to introduce alcohols selectively at the 3‐position of 3,4,5‐trifluoroaniline is described. The procedure uses powdered NaOH as... 
Arenes | Nucleophilic substitution | Aromatic substitution | Fluorine | ALKOXIDES | CHEMISTRY, ORGANIC | FLUOROBENZENES | FLUORIDES | SOLVENT | NUCLEOPHILIC AROMATIC-SUBSTITUTION | ETHERS | DISPLACEMENT | DERIVATIVES | Crown ethers | Toluene | Fluorides
Journal Article
The Journal of Organic Chemistry, ISSN 0022-3263, 09/2003, Volume 68, Issue 18, pp. 6984 - 6987
Nine 2,4-dioxo-2,3,4,5-tetrahydro-1H-pyrrolo[3,2-d]pyrimidine-6-carboxylic acid benzyl esters 12 were synthesized in four steps from 4-oxo-N-(PhF)proline... 
C-NUCLEOSIDES | RECEPTOR ANTAGONISTS | PURINE NUCLEOSIDE PHOSPHORYLASE | CHEMISTRY, ORGANIC | INHIBITORS | 9-DEAZAGUANINE | TRANSITION-STATE ANALOG | DERIVATIVES | Pyrimidines | Composition | Chemistry, Organic | Analysis | Substitution reactions | Ring formation (Chemistry) | Research | Nitrogen | Organic compounds
Journal Article
Tetrahedron, ISSN 0040-4020, 2004, Volume 60, Issue 50, pp. 11597 - 11612
In this paper, a synthetic approach for functionalised 5-aminopiperidinone-2-carboxylate (APC) systems as non-pro -peptide bond containing external β-turn... 
Diels–Alder reaction | Turn mimics | Pyrazinone | Diels-Alder reaction | PEPTIDE-BONDS | DIELS-ALDER REACTIONS | turn mimics | CHEMISTRY, ORGANIC | POLYPEPTIDES | STABILIZE SECONDARY STRUCTURES | GLY-PRO | 1,7-NAPHTHYRIDINE SCAFFOLD | AMINO-ACID DERIVATIVES | pyrazinone | 2(1H)-PYRAZINONES | GENERATION | CONFORMATIONAL-ANALYSIS
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 2001, Volume 42, Issue 33, pp. 5693 - 5695
Dichloropyrazinone 3 was converted into a conformationally restricted dipeptide analogue 8 by means of a Diels-Alder strategy. The β-turn characteristics of... 
pyrazinone | piperidinone | constrained dipeptide | Diels–Alder | β-turn mimic | Diels-Alder | Piperidinone | Constrained dipeptide | Pyrazinone | AMINO-ACID | PEPTIDES | DIELS-ALDER REACTIONS | CHEMISTRY, ORGANIC | beta-turn mimic | 2(1H)-PYRAZINONES
Journal Article
European Journal of Organic Chemistry, ISSN 1434-193X, 05/2003, Volume 2003, Issue 10, pp. 1868 - 1878
An intramolecular Diels−Alder strategy using 2(1H)‐pyrazinones was applied to generate a substituted perhydro‐1,7‐naphthyridine ring system that served as a... 
Conformation analysis | Naphthyridine | Bioorganic chemistry | Cycloaddition | Peptidomimetics | conformation analysis | DESIGN | naphthyridine | MIMETICS | DIELS-ALDER REACTIONS | CHEMISTRY, ORGANIC | NUCLEIC-ACIDS | cycloaddition | bioorganic chemistry | AMINO-ACIDS | FORCE-FIELD | peptidomimetics | 2(1H)-PYRAZINONES | PROTEINS | MOLECULAR MECHANICS
Journal Article
Tetrahedron, ISSN 0040-4020, 2003, Volume 59, Issue 26, pp. 4721 - 4731
Two analogues of formerly described piperidine-based Substance P antagonists have been synthesised using an intramolecular Diels-Alder reaction of... 
antagonists | pyrazinone | tachykinins | Substance P | intramolecular Diels–Alder | Intramolecular Diels-Alder | Antagonists | Tachykinins | Pyrazinone | intramolecular Diels-Alder | CHEMISTRY, ORGANIC | NEUROKININ RECEPTOR ANTAGONISTS | DISCOVERY | TACHYKININ RECEPTORS | NK1 ANTAGONISTS | HNK ANTAGONISTS | GAS-PHASE | substance P | BRAIN
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 2001, Volume 42, Issue 42, pp. 7397 - 7399
The intramolecular Diels-Alder reaction of three 1-(ω-alkenyl)-2(1H)-pyrazinones was investigated. Cycloaddition was shown to proceed for 1-(4-pentenyl)- and... 
CHEMISTRY, ORGANIC | 2(1H)-PYRAZINONES
Journal Article
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