Translational Drug Discovery Group


Trends in medicinal chemistry; Cowley, P., Hales, N., Ward, S; Drugs Fut 2011, 36(7): 543

Trends in Pain Research; R. Davenport, R. Armour and S. Ward; Drugs of the Future 2011, 36(12): 943-948

Ben A. Egan, Michael Paradowski, Rodolfo Marquez. Synthesis of the C1-C16 of (+)-Ajudazol A. Tetrahedron, 2011, 67(50), 9700-9707

Duncan Hay, Fiona M. Adam, Gerwyn Bish, Frederick Calo, Rachel Dixon, Jonathan Fray, James Hitchin, Peter Jones, Michael Paradowski, Gemma C. Parsons, Katie J.W. Proctor, David C. Pryde, Nicholas N. Smith and Thien-Duc Tran. A flexible synthesis of C-6 and N-1 analogues of a 4-amino-1,3-dihydroimidazo[4,5-c]pyridin-2-one core. Tetrahedron Letters, 2011, 52(44), 5728-5732

Charles E. Mowbray, Andrew S. Bell, Nicholas P. Clarke, Michelle Collins, Rhys M. Jones, Charlotte A.L. Lane, Wai L. Liu, Sandra D. Newman, Michael Paradowski, Emanuel J. Schenck, Mathew D. Selby, Nigel A. Swain and David H. Williams; Challenges of drug discovery in novel target space. The Discovery and Evaluation of PF-3893787: A Novel Histamine H4 Receptor Antagonist. Bioorganic & Medicinal Chemistry Letters, 2011, doi:10.1016/j.bmcl.2011.07.125 

Simon E. Ward, Mark Harries, Laura Aldegheri, Nigel E. Austin, Stuart Ballantine, Elisa Ballini, Daniel M. Bradley, Benjamin D. Bax, Brian P. Clarke, Andrew J. Harris, Stephen A. Harrison, Rosemary A Melarange, Claudette Mookherjee, Julie Mosley, Gianni Dal Negro, Beatrice Oliosi, Kathrine J. Smith, Kevin M. Thewlis, Patrick M. Woollard, Shahnaz P. Yusaf; Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators. Journal of Medicinal Chemistry, 2011, 54 (1), pp 78–94.



Fiona M. Adam, Gerwyn Bish, Frederick Calo, Christopher L. Carr, Nieves Castro, Duncan Hay, Paul B. Hodgson, Peter Jones, Craig J. Knight, Michael Paradowski, Gemma C. Parsons, Katie J. W. Proctor, David C. Pryde, Filippo Rota, Mya C. Smith, Nicholas Smith, and Thien-Duc Tran. Development of a Practical Synthesis of Toll-like Receptor Agonist PF-4171455: 4-Amino-1-benzyl-6-trifluoromethyl-1,3-dihydroimidazo [4,5-c] pyridin-2-one. Organic Process Research & Development, 2011, 45(4), 788-796.

Ben A. Egan, Michael Paradowski, Rodolfo Marquez. Regiocontrolled Rearrangement of Isobenzofurans. Organic Letters 2011, 13 (8), 2086-2089.

Michael Paradowski, Charlotte A. L. Lane, Torren Peakman. Synthesis of a novel octahydro pyrrolo[3,4-c] pyrrole cyclic amidine via 1,3-dipolar cycloaddition of azomethine ylides. Synlett, 2011, 11, 1543-1546.

David C. Pryde, Thien-Duc Tran, Peter Jones, Gemma C. Parsons, Gerwyn Bish, Fiona M. Adam, Mya C. Smith, Donald S. Middleton, Nick N. Smith, Frederick Calo, Duncan Hay, Michael Paradowski, Katie J. W. Proctor, Tanya Parkinson, Carl Laxton, David N. A. Fox, Nigel J. Horscroft, Giuseppe Ciaramella, Hannah M. Jones, Jonathan Duckworth, Neil Benson, Anthony Harrison and Rob Webster. The discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection. Med. Chem. Commun., 2011, 2 (3), 185-189.

Atack, J.R., GABAAreceptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics. Curr. Top. Med. Chem., 2011, 1176-1202.


Atack, J.R., GABA­A receptor subtype-selective modulators. II. α5-selective inverse agonists for cognition enhancement. Curr. Top. Med. Chem., 2011, 1203-1214.

Atack, J.R., Hallett, D., Tye, S., Wafford, K.A., Burns, H.D., Dawson, G.R., Street, L.J., McKernan, R.M., Pike, A., Agrawal, N.G.B., van Laere, K., Hargreaves, R.J. and Murphy, M.G. (2011a) Preclinical and clinical pharmacology of TPA023B, A GABAA receptor α2/α3 subtype-selective agonist. J. Psychopharmacol., 25:329-344.

Atack, J.R., Wafford, K.A., Street, L.J., Dawson, G.R., McKernan, R.M., Agrawal, N.G.B., van Laere, K., Burns, H.D., Murphy, M.G. and Hargreaves, R.J. (2011b) MRK-409, a GABAA receptor subtype-selective agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in man. J. Psychopharmacol., 25:315-328.

Fischer, B.D., Atack, J.R., Platt, D.M., Pike, A., Reynolds, D.S., Dawson, G.R. and Rowlett, J.K. Contribution of GABAA receptors containing a3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys. Psychopharmacol., 215:311-319.

Swanson, D.M., Wong, V.D., Jablonowski, J.A., Shah, C., Rudolph, D.A., Dvorak, C.A., Seierstad, M., Dvorak, L.K., Morton, K., Nepomuceno, D., Atack, J.R., Bonaventure, P., Lovenberg, T.W. and Carruthers, N.I. The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor. Bioorg. Med. Chem. Lett., 21:5552-5556.