Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Marzia Villa"'
Autor:
Eun Kyung Lee, Pravin Iyer, Sandra Steiner, Matthew C. Lucas, Ryan Craig Schoenfeld, Hai-Ying Cai, David S. Carter, Robert James Weikert, Marzia Villa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4630-4633
A variety of novel aminoheterocycle scaffolds as selective monoamine reuptake inhibitors have been prepared and one of these scaffolds is achiral. The main elements responsible for hERG channel, CYP2D6 and CYP3A4 inhibition were identified.
Publikováno v:
Tetrahedron. 61:10801-10810
The malfunctioning of protein kinases is a hallmark of numerous diseases, for which a satisfactory therapy is missing. We describe the design and synthesis of a kinase targeted library based on a novel 2-(3-phenyl-1H-pyrazol-4-yl)-1,3-benzoxazole sca
Publikováno v:
Organic & Biomolecular Chemistry. 1:247-250
A four step synthesis of 4(S)-oxazolidineacetic acid, 2-oxo benzyl ester (D-Oxac-OBn) from L-Asp-OH in 45% overall yield is reported. The formation of by-products is completely avoided, by microwave irradiation and by the use of caesium carbonate as
Autor:
Alessandra Barazza, Fernando Formaggio, Marco Crisma, Marzia Villa, Claudio Toniolo, Claudia Tomasini, Bernard Kaptein, Quirinus B. Broxterman, Herbert Mayrhofer, Cristina Peggion, Peter Pöchlauer
Publikováno v:
Journal of the Chemical Society, Perkin Transactions 2. :644-651
By a chemo-enzymatic approach we performed a large-scale, stereoselective synthesis of the Cα-methylated α-hydroxy acid L-(αMe)Hyv. We also prepared model depsipeptides based on this sterically demanding residue in combination with the α-amino ac
Publikováno v:
Tetrahedron. 55:8103-8110
The diastereoselective addition of higher order (H.O.) cuprates and zinc-copper reagents to aliphatic and aromatic chiral imines derived from ( S )-1-phenylethylamine was examined. Aliphatic chiral imines react with (Allyl) 2 CuCNLi 2 and (n-Bu) 2 Cu
Publikováno v:
ChemInform. 29
A general approach to the solution phase parallel synthesis of perhydrooxazin-4-ones, which allows the preparation of milligram quantities of each individual member, is reported. An efficient purification method, using as “Sequestration Enabling Re
Publikováno v:
ChemInform. 29
Publikováno v:
ChemInform. 30
The diastereoselective addition of higher order (H.O.) cuprates and zinc-copper reagents to aliphatic and aromatic chiral imines derived from ( S )-1-phenylethylamine was examined. Aliphatic chiral imines react with (Allyl) 2 CuCNLi 2 and (n-Bu) 2 Cu
Autor:
Anthony W. Thompson, Shelley K. Gleason, David S. Carter, Michael Patrick Dillon, Yansheng Zhai, Anthony P.D.W. Ford, Joel R Gever, Amy Geraldine Moore, Christine E. Brotherton-Pleiss, Clara Jeou Jen Lin, Marzia Villa
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(3)
Despite the extensive literature describing the role of the ATP-gated P2X 3 receptors in a variety of physiological processes the potential of antagonists as therapeutic agents has been limited by the lack of drug-like selective molecules. In this pa
Autor:
Eun Kyung Lee, Ralf Roetz, Clara Jeou Jen Lin, Jason Choy, Amy Geraldine Moore, Sandra Steiner, Kerem Erol Ozboya, Yansheng Zhai, Robert James Weikert, Karin Ann Stein, David S. Carter, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Pravin Iyer, Hai-Ying Cai, Saul Jaime-Figueroa, Robert Greenhouse, Lubica Raptova, Ryan Craig Schoenfeld, Linda M. Bannwart, Marzia Villa
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(23)
A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro microsomal stability and in vitro permeability, and low drug-drug interaction potential are desc