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Christoph W. Zapf
Researcher at Pfizer
Publications - 27
Citations - 846
Christoph W. Zapf is an academic researcher from Pfizer. The author has contributed to research in topics: Peptidomimetic & Hepatitis C virus. The author has an hindex of 14, co-authored 27 publications receiving 783 citations. Previous affiliations of Christoph W. Zapf include Princeton University & University of California, San Diego.
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Journal ArticleDOI
Diprotected Triflylguanidines: A New Class of Guanidinylation Reagents
Journal ArticleDOI
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design
Katherine L. Lee,Catherine M. Ambler,David R. Anderson,Brian P. Boscoe,Andrea G Bree,Joanne Brodfuehrer,Jeanne S. Chang,Chulho Choi,Seung Won Chung,Kevin J. Curran,Jacqueline E. Day,Christoph Martin Dehnhardt,Ken Dower,Susan E. Drozda,Richard K. Frisbie,Lori Krim Gavrin,Joel Adam Goldberg,Seungil Han,Martin Hegen,David Hepworth,Heidi R. Hope,Satwik Kamtekar,Iain Kilty,Arthur Lee,Lih-Ling Lin,Frank Lovering,Michael Dennis Lowe,Mathias John Paul,Heidi M. Morgan,Elizabeth Murphy,Nikolaos Papaioannou,Akshay Patny,Pierce Betsy S,Vikram R. Rao,Eddine Saiah,Ivan J. Samardjiev,Brian Samas,Marina W.H. Shen,Julia H Shin,Holly H. Soutter,Strohbach Joseph Walter,Peter T. Symanowicz,Jennifer R. Thomason,John David Trzupek,Richard Vargas,Fabien Vincent,Jiangli Yan,Christoph W. Zapf,Stephen W. Wright +48 more
TL;DR: The medicinal chemistry effort featured the judicious placement of lipophilicity, informed by co-crystal structures with IRAK4 and optimization of ADME properties to deliver clinical candidate PF-06650833 (compound 40), which displays a 5-unit increase in lipophilic efficiency from the fragment hit, excellent kinase selectivity, and pharmacokinetic properties suitable for oral administration.
Journal ArticleDOI
A Diels-Alder macrocyclization enables an efficient asymmetric synthesis of the antibacterial natural product abyssomicin C.
Journal ArticleDOI
Covalent inhibitors of interleukin-2 inducible T cell kinase (itk) with nanomolar potency in a whole-blood assay.
Christoph W. Zapf,Brian S. Gerstenberger,Li Xing,David C. Limburg,David R. Anderson,Nicole Caspers,Seungil Han,Ann Aulabaugh,Ravi G. Kurumbail,Subarna Shakya,Xiangping Li,Spaulding,Robert M. Czerwinski,Nilufer P. Seth,Quintus G. Medley +14 more
TL;DR: Structural-based drug design was utilized to achieve low nanomolar potency of the disclosed series even at high ATP concentrations, and prolonged effect indicates that covalent inhibition is a viable strategy to target the inactivation of Itk.
Journal ArticleDOI
New reagents, reactions, and peptidomimetics for drug design.
TL;DR: The reagent 3-(diethoxyphosphoryloxy)-1,2,3-benzotriazin-4(3H)-one for amide bond formation to couple sterically hindered structures and these couplings proceed with remarkably strong resistance to racemization.