Brown A.,Pfizer |
Ellis D.,Pfizer |
Favor D.A.,Shanghai Chempartner |
Kirkup T.,St Anslems RC Secondary School |
And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2013
A new series of 2-(benzyloxy)benzamides are presented that are potent functional antagonists of TRPM8 and possess improved LipE and LE compared to the original lead. They were discovered through a series of compound libraries and we present a powerful visualization method for the chemical space explored with each library. Remarkably this new series originated from the highest risk design strategy where compounds were synthesised with the least degree of similarity to the lead structure. © 2013 Elsevier Ltd. All rights reserved.
Harker W.R.R.,University of Sheffield |
Delaney P.M.,Peakdale Molecular |
Simms M.,Peakdale Molecular |
Tozer M.J.,Peakdale Molecular |
Harrity J.P.A.,University of Sheffield
Tetrahedron | Year: 2013
The multigram synthesis of N-protected 2-pyridone boronic acid derivatives via a [4+2] cycloaddition of alkynylboronates with 2-pyrazinones is presented. The reactions are highly chemoselective, and generally highly regioselective although trimethylsilyl-substituted alkynylboronates have proven to be an exception. Nonetheless, in this latter case, separation of regioisomers was successfully accomplished via high performance counter-current chromatography allowing isolation of analytically pure 2-pyridones. Further derivatisations of trimethylsilyl-substituted 2-pyridone boronates were performed providing access to a selection of functionalised scaffolds. © 2012 Published by Elsevier Ltd.
Betson M.,Peakdale Molecular |
Allanson N.,Peakdale Molecular |
Wainwright P.,Peakdale Molecular
Organic and Biomolecular Chemistry | Year: 2014
Modified nucleosides have received a great deal of attention from the scientific community, either for use as therapeutic agents, diagnostic tools, or as molecular probes. Perhaps the most difficult position of a nucleoside to modify is the 4′-position. Chemists have developed innovative methods to achieve this in a stereoselective manner to allow incorporation of a variety of functional groups. This review provides a summary of the most commonly used or recently published methods for ribose, deoxy-ribose, 4′-thioribose, and carbocyclics. This journal is © The Royal Society of Chemistry 2014.