Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Kay Brickmann"'
Autor:
Michael O'sullivan, Kay Brickmann, Peter Bach, Jonas Boström, Darren Martin Harvey, Robert D. Groneberg, J.J.J. van Giezen, Fredrik Zetterberg
Publikováno v:
European Journal of Medicinal Chemistry. 65:360-375
The present paper describes the development of a new series of P2Y12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC50 binding affinity = 0.33 μM, aq solubility
Autor:
J.J.J. van Giezen, Jonas Boström, Kay Brickmann, Fredrik Zetterberg, Ragnar Hovland, Peter Bach, Asim K. Ray, Annika U. Petersson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2877-2881
A novel series of P2Y12 antagonists for development of drugs within the antiplatelet area is presented. The synthesis of the piperazinyl-pyridine urea derivatives and their structure–activity relationships (SAR) are described. Several compounds sho
Publikováno v:
Tetrahedron. 62:10937-10944
A synthetic route to a 2,4-disubstituted pyridine as a potential β-strand mimetic has been developed and applied in the synthesis of a tripeptidomimetic of Leu-Gly-Gly. The pyridine scaffold replac ...
Publikováno v:
Liebigs Annalen. 1996:457-471
Publikováno v:
The Journal of Organic Chemistry. 69:3500-3508
A beta-turn mimetic in which the four amino acids of a beta-turn have been replaced by a 10-membered ring has been designed, synthesized, and subjected to conformational studies. In the mimetic, the intramolecular CO(i)-HN(i)(+3) hydrogen bond that i
Autor:
Jan Kihlberg, Kjell Ekholm, ZhongQing Yuan, Birgitta Johansson, and Anders Nilsson, Ingmar Sethson, Kay Brickmann, David Blomberg
Publikováno v:
Journal of Medicinal Chemistry. 45:2512-2519
Oxytocin is a neurohypophyseal peptide hormone that induces labor and lactation in mammals. An inverse gamma-turn mimetic corresponding to the tripeptide Ile-Val-Asn has been synthesized and incorporated instead of residues 3-5 of oxytocin to probe t
Publikováno v:
Chemistry - A European Journal. 5:2241-2253
Peptidesecondarystructuremimetics should accurately imitate the desired backbone conformation, and synthetic routes to peptidomimetics should allow for flexible introduction of side chains with correct stereochemistry. Both criteria are met by the en
Autor:
Peter, Bach, Jonas, Boström, Kay, Brickmann, J J J, van Giezen, Robert D, Groneberg, Darren M, Harvey, Michael, O'Sullivan, Fredrik, Zetterberg
Publikováno v:
European journal of medicinal chemistry. 65
The present paper describes the development of a new series of P2Y12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC50 binding affinity = 0.33 μM, aq solubility0.1 μM, microsomal CLint (HLM) ≥300 μM/min/mg). B
Publikováno v:
Chemische Berichte. 127:1949-1957
The nBuLi-induced tin/lithium exchange reactions of the di-astereomeric γ-[(methoxyethoxy)methoxy]-]α-(tributylstannyl) sulfides anti- and syn-8 delivered the α-(lithioalkyl) benzyl sulfides anti- and syn-11, respectively. Within 1 h at -78°C, th
Autor:
Emre M. Isin, David Blomberg Saitton, Eric Wellner, Rutger H. A. Folmer, Pernilla Ståhlberg, Kay Brickmann, Volker Schnecke, Öjvind Davidsson, Christoffer Bengtsson, Lars-Olof Larsson, Stefan Hallén, Pernilla Sörme, Hong Wan, Kenth Hallberg, Linda Öster, Ragnar Hovland, Lars Löfgren, Alleyn T. Plowright, Bengt Kull, Tobias Noeske, Stefan Blaho, Petra Johannesson, Tomas Drmota, Kristina Nilsson, Johan Broddefalk, Nick Oakes
Publikováno v:
Bioorganicmedicinal chemistry. 19(10)
Inhibition of acetyl-CoA carboxylases has the potential for modulating long chain fatty acid biosynthesis and mitochondrial fatty acid oxidation. Hybridization of weak inhibitors of ACC2 provided a novel, moderately potent but lipophilic series. Opti