Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Rachel L. Eastwood"'
Autor:
Rachel L. Eastwood, Kerry A. Paradowski, Donald Stuart Middleton, Jean-Yves Chiva, Barber Christopher Gordon, David C. Blakemore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1499-1503
Optimisation of a series of 4-piperidinyltriazoles led to the identification of compound 28a which showed good whole cell antiviral activity, excellent selectivity over the hERG ion channel and complete oral absorption.
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:
Rachel L. Eastwood, Barber Christopher Gordon, Kerry A. Paradowski, Michelle Y. Platts, David R. Fenwick, Jean-Yves Chiva, David C. Blakemore
Publikováno v:
Tetrahedron Letters. 52:512-514
An efficient route to dipyridone acid HIV integrase inhibitors is developed. The key steps include a one-pot three-step formation of the core template (containing one point of structural diversity) followed by a regioselective benzylation and in situ
Autor:
Rachel L. Eastwood, Donald Stuart Middleton, David C. Blakemore, Barber Christopher Gordon, Jean-Yves Chiva, Kerry A. Paradowski
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(4)
The development of a new class of CCR5 antagonist replacing the tropane core of maraviroc by piperidine with a branched N-substituent is described. Compound 15h shows good whole cell antiviral activity together with microsomal stability and only weak