Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Helen J. Mason"'
Autor:
James Edward John Mills, Thomas Ryckmans, Christelle Pasquinet, Patrick S. Johnson, Dave J. Rawson, Mark L. Lewis, Lee R. Roberts, Toby J. Underwood, Simon Wheeler, Helen J. Mason, Rachel Jane Russell, Julie Newman, David M. Beal, Dack Kevin Neil, Deborah Spark, Robin Ward, Alan Stobie, Neil Feeder, Anthony Harrison, Justin Stephen Bryans
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5684-5687
The V1a receptor has emerged as an attractive target for a range of indications including Raynaud's disease and dysmenorrhoea. As part of an effort to discover a new class of orally active V1a antagonist, we optimised a highly lipophilic, metabolical
Autor:
Manos Perros, David C. Pryde, Rob Webster, Francesca Perruccio, Michelle Y. Platts, Rhys M. Jones, Deborah Rodrigues, David V. Batchelor, David Ellis, Donald Stuart Middleton, David R. Fenwick, Patrick Dorr, Stupple Paul Anthony, Mike Westby, Anthony Wood, Helen J. Mason, Nicholas Smith, Martin Corless, Sebastien Galan, Peter T. Stephenson
Publikováno v:
Journal of Medicinal Chemistry. 54:67-77
Preventing entry of HIV into human host cells has emerged as an attractive approach to controlling viral replication. Maraviroc 1 is an approved antagonist of the human CCR5 receptor which prevents the entry of HIV. Herein, we report the design and d
Autor:
Gemma C. Parsons, Peter T. Stephenson, Michelle Y. Platts, Barber Christopher Gordon, Blanda Luzia Christa Stammen, David C. Pryde, David Ellis, David W. Gordon, Helen J. Mason, Rachel L. Eastwood, Catherine Burt, Donald Stuart Middleton, David Bachelor, Martin Corless, Keith Statham, Anthony Wood, Wolfgang Klute, Kerry A. Paradowski, David C. Blakemore, David R. Fenwick
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1084-1088
The synthesis of a range of novel amine-containing structures and their primary potency as inhibitors of HIV-1 fusion via blocking of the CCR5 receptor is described. The development of the medicinal chemistry strategy and SAR's which led to the ident
Autor:
Laurie Seliger, Jian Wang, Ronald Pongrac, Helen J. Mason, Bruce Beyer, Andrew Henwood, John Krupinski, Ximao Wu, John E. Macor, Saeho Chong, Rongan Zhang, Pam Ferrer, Diane E. Normandin, Guixue Yu, Leonard P. Adam, William G. Humphrey, Bin He
Publikováno v:
Journal of Medicinal Chemistry. 46:457-460
Novel pyrazolopyridopyridazine derivatives have been prepared as potent and selective PDE5 inhibitors. Compound 6 has been identified as a more potent and selective PDE5 inhibitor than sildenafil (1). It is as efficacious as sildenafil in in vitro an
Autor:
Ximao Wu, Helen J. Mason, Michael Witkus, John E. Macor, William R. Ewing, Guixue Yu, Kim Galdi, Ning Zhao, Cornelius Lyndon A M
Publikováno v:
Synthesis. 2003:0403-0407
Sulfuryl chloride has been used to mono-chlorinate electron-rich arylalkyl- and heteroarylalkyl-amines and amino acids in a mild and efficient one-pot transformation with straightforward purification. Protection of the amines was not needed, and race
Publikováno v:
Tetrahedron Letters. 42:8931-8934
Hetero Diels–Alder reactions of heteroaromatic amidines and maleimide afforded novel fused pyridopyrrolidine dione scaffolds in moderate to good yields under mild conditions.
Publikováno v:
Tetrahedron Letters. 51:2849-2851
This Letter outlines a new two-step process for the synthesis of 4-fluoropyrazole and its application in an improved synthesis of 4-fluoro-1-[5-fluoro-1-(1H-imidazol-2-yl)-indan-4-ylmethyl]-1H-pyrazole. The original synthesis of 4-fluoro-1-[5-fluoro-
Autor:
Mark L. Lewis, Kana Kon-I, Dafydd R. Owen, Tim Young, Mifune Takeuchi, Isabelle Tran, Miyako Matsumizu, Denise Harding, Helen J. Mason, Christine Anne Louise Watson, Akiko Shima, Margarita Rodriguez-Lens, Takasuke Mukaiyama
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(14)
A series of benzimidazole CB2 receptor agonists were prepared and their properties investigated. Optimisation of the three benzimidazole substituents led to the identification of compound 23, a potent CB2 full agonist (EC50 2.7 nM) with excellent sel
Publikováno v:
Tetrahedron Letters. 42:3247-3249
Sulfuryl chloride was used to chlorinate electron-rich arylalkyl amines in a mild and efficient one-pot transformation with simple product isolation via precipitation. Protection of the amine was not needed.
Autor:
John Krupinski, Saeho Chong, Andrew Henwood, Ximao Wu, Leonard P. Adam, Guixue Yu, Jian Wang, Ronald Pongrac, John E. Macor, Bin He, Gary Dorough, Diane E. Normandin, Helen J. Mason, Laurie Seliger
Publikováno v:
Journal of Medicinal Chemistry. 44:1025-1027