Mark E. Webster
Procter & Gamble
9 Papers
41 Citations
Mark E. Webster is an academic researcher from Procter & Gamble. The author has contributed to research in topics: Chemical synthesis & Tachykinin receptor. The author has an hindex of 7, co-authored 9 publications.
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Papers
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).
Michael P. Clark,Kelly M. George,Roger G. Bookland,Jack J. Chen,Steven K. Laughlin,Kumar D. Thakur,Wenlin Lee,Jan Richard Davis,Ed J. Cabrera,Todd A. Brugel,John C. VanRens,Matthew J. Laufersweiler,Jennifer A. Maier,Mark Sabat,Adam Golebiowski,Vijay Easwaran,Mark E. Webster,Biswanath De,George Zhang +18 more
TL;DR: A new class of bicyclic pyrrolopyrimidine-based Janus kinase 3 (JAK-3) inhibitors are described and many of these inhibitors showed low nanomolar activity against Jak-3.
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Identification and chemical synthesis of mdl 105,212, a non-peptide tachykinin antagonist with high affinity for nk1 and nk2 receptors
Burkholder Timothy P,Kudlacz Elizabeth M,Tieu-Binh Le,Robert W. Knippenberg,S. A. Shatzer,Maynard George D,Mark E. Webster,Stephen W. Horgan +7 more
TL;DR: MDL 105,212 is synthesized and identified, a non-peptide tachykinin receptor antagonist that has high affinity for human NK1 and NK2 receptors.
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Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists
Burkholder Timothy P,Kudlacz Elizabeth M,Maynard George D,Xiao-Gao Liu,Tieu-Binh Le,Mark E. Webster,Stephen W. Horgan,David L. Wenstrup,David W. Freund,Fred E. Boyer,Larry D. Bratton,Raymond S. Gross,Robert W. Knippenberg,Deborah E. Logan,Bryan K. Jones,Teng-Man Chen,Julie L. Geary,Melinda A. Correll,J. Chuck Poole,Arun K. Mandagere,Thomas N. Thompson,Kin-Kai Hwang +21 more
TL;DR: The synthesis and structure-activity relationships for a series of analogs of MDL 105,212 with regards to NK1 and NK2 receptor binding affinity, physical-chemical characterization, in vitro absorption potential; in vitro metabolic stability; and efficacy in a capsaicin-challenge conscious guinea pig model after oral administration are reported.
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Discovery of Orally Bioavailable 1,3,4-Trisubstituted 2-Oxopiperazine-Based Melanocortin-4 Receptor Agonists as Potential Antiobesity Agents
Xinrong Tian,Adrian Gregory Switzer,Steve A. Derose,Rajesh K. Mishra,Mark Gregory Solinsky,Mumin Rashid Naeem,Frank H. Ebetino,Lalith R. Jayasinghe,Mark E. Webster,Anny-Odile Colson,Doreen Crossdoersen,Beth B. Pinney,Julie A. Farmer,Martin E. Dowty,Cindy Obringer,Charles A. Cruze,Melissa L. Burklow,Paula M. Suchanek,Lily Dong,Mary Kay Dirr,Russell James Sheldon,John August Wos +21 more
TL;DR: A study that was designed to identify plausible replacements for highly basic guanidine moiety contained in potent MC4R agonists led to the discovery of initial nonguanidine lead 5, and it is demonstrated that compound 35 showed promising oral bioavailability and a moderate oral half life and induced significant weight loss in a 28-day rat obesity model.
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Hydroxyoxazolidines as α-aminoacetaldehyde equivalents: Novel inhibitors of calpain
Norton P. Peet,Hwa-Ok Kim,Angela L. Marquart,Michael R. Angelastro,Nieduzak Thaddeus R,Julie N. White,Dirk Friedrich,Gary A. Flynn,Mark E. Webster,Roy J. Vaz,Matthew D Linnik,Koehl Jack Roger,Shujaath Mehdi,Philippe Bey,Bart Emary,Kin-Kai Hwang +15 more
TL;DR: In this paper, the synthesis of [1]-(5-hydroxy-4-(phenylmethyl)-3-oxazolidinyl)carbonyl]-2-ethylpropyl] carbamic acid phenylmethyl ester (2; MDL 104,903), a potent inhibitor of calpain, is described.
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