Zobrazeno 1 - 10 of 14 pro vyhledávání: '"Scott F. Leonard"'
1
Hit to Lead Account of the Discovery of a New Class of Inhibitors of Pim Kinases and Crystallographic Studies Revealing an Unusual Kinase Binding Mode
Autor: Eugene R. Hickey, Anthony S. Prokopowicz, George E. Lee, Carol Ann Homon, Scott Jakes, Wang Mao, Jun Li, Charlene Peng, Bennett T. Farmer, Scott F. Leonard, Mohammed A. Kashem, Kevin Chungeng Qian, Charles L. Cywin, Lian Wang, Ronald Magboo, Morgan Welzel, John P. Wolak, Edward Pack, Tina Morwick
Publikováno v: Journal of Medicinal Chemistry. 52:1814-1827
A series of inhibitors of Pim-2 kinase identified by high-throughput screening is described. Details of the hit validation and lead generation process and structure-activity relationship (SAR) studies are presented. Disclosure of an unconventional bi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40bdff6788836da6a99ef9f5bd96cab0
https://doi.org/10.1021/jm801242y
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2
Diverse 2-Carboxamide-3-amino-Substituted Quinoxalines: Synthesis and Reactivity Investigation for Library Generation
Autor: Scott F. Leonard, George E. Lee, Jennifer A. Kowalski
Publikováno v: Journal of Combinatorial Chemistry. 8:774-779
Described herein is the development of a robust synthetic route applicable to parallel synthesis of diverse 2-carboxamide-3-amino-substituted quinoxalines. In addition to the scope and limitations of the methods developed, a purification strategy emp
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52aa2230e7454363c30b6110c6363eb3
https://doi.org/10.1021/cc060058v
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3
Solution conformation of the ketone and epoxide synthetic precursors of β-chamigrene determined by1H and13C NMR spectroscopy and distance geometry
Autor: T. Phil Pitner, Scott F. Leonard, Denice M. Spero, Paul-James Jones
Publikováno v: Magnetic Resonance in Chemistry. 31:906-909
Utilizing 2D NMR spectroscopy (COSY, NOESY, TOCSY, inverse detected 1 H/ 13 C correlation spectroscopy), the 1 H and 13 C NMR spectra of the ketone and epoxide precursors of β-chamigrene were assigned. The dihedral angles and distances determined fr
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bb99862e054d6621516d3425b550ce5a
https://doi.org/10.1002/mrc.1260311006
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4
A novel stereoselective route to (S)-(+)-.alpha.-(fluoromethyl)histidine: .alpha.-halomethylation of (2R,4S)-3-benzoyl-2-(1,1-dimethylethyl)-1-methyl-4-[(N-tritylimidazol-4-yl)methyl]-1,3-imidazolidin-5-one. Synthesis and proton NMR spectroscopy
Autor: Richard W. Kriwacki, Karl G. Grozinger, T. Phil Pitner, Scott F. Leonard
Publikováno v: The Journal of Organic Chemistry. 58:709-713
A method is described for the α-enantioretentive methylation of L-histidine (S) to give (S)-(+)-α-(fluoromethyl)histidine (8). The synthesis involves the conversion of N im -trityl-L-histidine methyl ester (1) to both the «trans»-(2S,4S)- and «c
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0216886fe0bc7f080990884267922170
https://doi.org/10.1021/jo00055a027
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6
ChemInform Abstract: Imidazo(1,2-a)piperazines as Mechanistic Inhibitors of Serine Proteinases
Autor: Scott F. Leonard, Victor Fuchs, Jerry W. Skiles
Publikováno v: ChemInform. 23
The synthesis of imidazo[1,2-a]piperazines bearing a trifluoromethyl substituent, potential inhibitors of serine proteinases, is illustrated.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::acf23a0097c3597d9e91e4b931f147e9
https://doi.org/10.1002/chin.199239219
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8
Imidazo[1,2-a]piperazines as mechanistic inhibitors of serine proteinases
Autor: Scott F. Leonard, Jerry W. Skiles, Victor Fuchs
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 1:69-72
The synthesis of imidazo[1,2-a]piperazines bearing a trifluoromethyl substituent, potential inhibitors of serine proteinases, is illustrated.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::57fffcccfe9a2521765bff5017c9e962
https://doi.org/10.1016/s0960-894x(01)81094-5
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9
Amidomethylation of indoles and cyclisations to spiro[pyrrolo[4,3,2-de]isoquinoline-3,4′-piperidines]
Autor: Christine Carter, Kurt Freter, T. Phil Pitner, Scott F. Leonard, Richard W. Kriwacki
Publikováno v: Journal of Heterocyclic Chemistry. 24:387-391
Reactions de chloroacetylaminomethyl-4 indoles (prepares par amidomethylation des methoxy-5 methyl-2 et trimethyl-2,5,6 indoles) avec la N-acetyl piperidone-4 ou des derives du benzaldehyde: obtention de spiro [piperidine-4:3'-pyrrolo [4,3,2-de] isoq
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::94e1a20b99ec524b8803fcca7afd1ad1
https://doi.org/10.1002/jhet.5570240218
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