Publications

A full list of publications:

Patents

  • 83 patent applications

Presentations

  • Driving For Success In Lead Optimization Select Biosciences Outsourcing Conference Munich 9th April 2010
  • Living in the Free Lane Some recent perspectives on CNS Drug Discovery 23rd April 2010 Kings College BBB Club, London
  • Challenges for Medicinal Chemists in Successful and Effective Collaborations & Partnerships in Drug Discovery Select Biosciences Outsourcing Conference Meeting London June 2009
  • GlyT-1 Inhibitors: from Tools to PETs, ACS, Philadelphia, Aug 2008.
  • Symposium session featured in C&E News 15th September 2008.
  • Quinoline ureas as Orexin-1 receptor antagonists; Advances in Neurochemistry February 2001.
  • Quinoline ureas as Orexin-1 receptor antagonists; Italian Med Chem summer school 2000.
  • SB-209509 a novel 5-HT1D agonist for the treatment of migraine; SMR Case Histories Meeting 1995.

Posters

  • Two posters presented at external meetings.
  • Three posters presented at internal meetings.

Papers and book chapters

  1. R. J. R. Elliott et al Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors MedChemComm 2015,6, 1687.
  2. Roderick A Porter and Lee A Dawson GlyT-1 Inhibitors: From Hits to Clinical Candidates Ed S. Celanire and S. Poli Topics in Medicinal Chemistry, 2014 Springer-Verlag, Berlin, Heidelberg (available on line)
  3. S. P. Collingwood, A. J. Ratcliffe and R. Porter From Targets to Candidates: Emerging Strategies in Drug Discovery Highlights from the Society of Medicines Research Symposium 12th Dec 2013 National Heart and Lung Institute London Drugs of the Future 2014, 39(2) 147
  4. Lee Dawson and Roderick A Porter Progress in the Development of Neurokinin 3 Modulators for the Treatment of Schizophrenia: Molecule Development and Clinical Progress Future Medicinal Chemistry 2013, 5, 1525
  5. Richard Blunt, Roderick Porter, Amanda Johns, David Nash, Gemma Puckey, Paul Wyman, Hugh Herdon, Simon Teague, Victoria Hadden, Stefano Fontana, Laurie Gordon Acylglycinamides as inhibitors of glycine transporter type 1 Bioorg. Med. Chem. Lett 2011, 21, 6176
  6. Romano Di Fabio , Annalisa Pellacani, Stefania Faedo, Adelheid Roth, Laura Piccoli, Philip Gerrard, Rod A. Porter, Christopher N. Johnson, Kevin Thewlis, Daniele Donati, Luigi Stasi, Simone Spada, Geoffrey Stemp, David Nash, Clive Branch, Leanda Kindon, Mario Massagrande, Alessandro Poffe, Simone Braggio, Elisabetta Chiarparin, Carla Marchioro, Emiliangelo Ratti and Mauro Corsi Discovery Process and Pharmacological Characterization of a Novel Dual Orexin 1 and Orexin 2 Receptor Antagonist Useful for Treatment of Sleep Disorders Bioorganic & Medicinal Chemistry Letters 2011, 21, 5562
  7. Hugh J. Herdon, Jennifer C. Roberts, Steve Coulton and Rod A. Porter Pharmacological characterisation of the GlyT-1 glycine transporter using two novel radioligands Neuropharmacology 2010, 59, 558
  8. Mikhail Kalinichev, Kathryn R. Starr, Simon Teague, Andrea M. Bradford, Rod A. Porter, Hugh J. Herdon  Glycine transporter 1 (GlyT1) inhibitors exhibit anticonvulsant properties in the rat maximal electroshock threshold (MEST) test, Brain Research, 2010, 1331, 105-113
  9. J. Passchier, G. Gentile, R. Porter, H. Herdon, C. Salinas, S. Jakobsen, H. Audrain, M. Laruelle, R.N. Gunn; Identification and evaluation of [11C]GSK931145 as a novel ligand for imaging the type 1 glycine transporter with positron emission tomography Synapse:542-549, 64, 2010
  10. Jeanette Watson, Sara Wright, Adam Lucas, Kirsten L. Clarke, Jean Viggers, Sharon Cheetham, Phil Jeffrey, Rod Porter, and Kevin D. Read Receptor Occupancy and Brain Free Fraction, Drug Metab. Dispos. 2009 37: 753-760
  11. W. Smith, Paul A. Wyman, Peter Lovell, Caroline Goodacre, Halina T. Serafinowska, Antonio Vong, Frank Harrington, Sean Flynn, Daniel M. Bradley, Rod Porter, Sara Coggon, Graham Murkitt, Kirsten Searle, David R. Thomas, Jeannette M. Watson, William Martin, Zining Wu and Lee A. Dawson; New quinoline NK3 receptor antagonists with CNS activity Bioorg Med. Chem.Lett 2009, 19, 837-840
  12. S. G. Summerfield;  A. J. Lucas;  R. A. Porter;  P. Jeffrey;  R. N. Gunn;  K. R. Read;  A. J. Stevens;  A. C. Metcalf;  M. C. Osuna;  P. J. Kilford;  J. Passchier; A. D. Ruffo  Toward an improved prediction of human in vivo brain penetration Xenobiotica (2008), 38(12), 1518 – 1535
  13. Summerfield, Scott G.; Read, Kevin; Begley, David J.; Obradovic, Tanja; Hidalgo, Ismael J.; Coggon, Sara; Lewis, Ann V.; Porter, Rod A.; Jeffrey, Phil.   Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction.    Journal of Pharmacology and Experimental Therapeutics  (2007),  322(1),  205-213.
  14. Rahman, Shahzad S.; Coulton, Steven; Herdon, Hugh J.; Joiner, Graham F.; Jin, Jian; Porter, Roderick A.. 1,3-Diaminopropan-2-ol Sulfonamides as potent and selective inhibitors of the glycine transporter type 1.  Bioorganic & Medicinal Chemistry Letters  2007,  17(6),  1741-1745
  15. Ishii, Y.; Blundell, J. E.; Halford, J. C. G.; Upton, N.; Porter, R.; Johns, A.; Rodgers, R. J. Satiety enhancement by selective orexin-1 receptor antagonist SB-334867: influence of test context and profile comparison with CCK-8S.  Behavioural Brain Research  2005,  160(1),  11-24
  16. Ishii, Y.; Blundell, J. E.; Halford, J. C. G.; Upton, N.; Porter, R.; Johns, A.; Jeffrey, P.; Summerfield, S.; Rodgers, R. J,  Anorexia and weight loss in male rats 24h following single dose treatment with orexin-1 receptor antagonist SB-334867. Behavioural Brain Research  (2005),  157(2),  331-341
  17. Ishii, Y.; Blundell, J. E.; Halford, J. C. G.; Upton, N.; Porter, R.; Johns, A.; Rodgers, R. J.  Differential effects of the selective orexin-1 receptor antagonist SB-334867 and lithium chloride on the behavioural satiety sequence in rats.    Physiology & Behavior  2004,  81(1),  129-140
  18. Langmead, Christopher J.; Jerman, Jeffrey C.; Brough, Stephen J.; Scott, Claire; Porter, Rod A.; Herdon, Hugh J.  Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.    British Journal of Pharmacology  2004,  141(2),  340-346.
  19. C. M. Marson, A. Khan, Rod. A. Porter and A. Cobb Functionalised Medium Rings by Stereospecific Expansions of 2,3-Epoxy alcohols under mild conditions Tetrahedron Letters  2002,  43(37),  6637-6640
  20. Marson, Charles M.; Khan, Afzal; Porter, Rod A.; Cobb, Alexander J. A.  Construction of functionalized medium rings by stereospecific expansions of 2,3-epoxy alcohols under mild conditions.    Tetrahedron Letters  2002,  43(37),  6637-6640.
  21. Marson, Charles M.; Khan, Afzal; Porter, Rod A..  Stereocontrolled Formation of Epoxy Peroxide Functionality Appended to a Lactam Ring.    Journal of Organic Chemistry  2001,  66(14),  4771-4775.
  22. R.J. Rodgers, J. C. G. Halford, R. L Nunes de Souza, A. L. Canto de Souza D. C. Piper, J. S Arch, N. Upton, R. A. Porter, A. Johns abnd J. E. Blundell SB-334867, a selective Orexin-1 receptor antagonist enhances  behavioural satiety and blocks the hyperphagic effect of Orexin-A in rats. E. Journal of Neuroscience 2001, 13, 1444
  23. J. G. Darker, R. A. Porter, D. S. Eggleston, D. Smart, S. J. Brough, C. Sabido-David and J. C. Jerman Structure-Activity analysis of Truncated Orexin-A analogues at the Orexin-1 receptor Bioorg. Med. Chem. Letters 2001, 11, 737.
  24. Smart, D.; Sabido-David, C.; Brough, S. J.; Jewitt, F.; Johns, A.; Porter, R. A.; Jerman, J. C.  SB-334867-A: the first selective orexin-1 receptor antagonist.    British Journal of Pharmacology  2001,  132(6),  1179-1182
  25. Porter, RA, Chan, WN, Coulton, S, Johns, A, Hadley, MS, Widdowson, K, Jerman, JC, Brough, SJ, Coldwell, M, Smart, D, Jewitt, F, Jeffrey, P, Austin, N  1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor. Bioorg. Med. Chem. Lett. 2001, 11, 1907-1910.
  26. Duxon MS, Stretton J, Starr K, Jones DNC, Holland V, Riley G, Jerman J, Brough S, Smart D, Johns A, Chan W, Porter R, and Upton, N.  Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX1) receptors, with downstream 5-HT2C receptor involvement. Psychopharmacology, 2001, 153, 203-209.
  27. Jones, DNC, Gartlon, J, Parker, F, Taylor, SG, Routledge, C, Hemmati, P, Munton, RP, Ashmeade, TE, Hatcher, JP, Johns, A, Porter, RA, Hagan, JJ, Hunter, AJ, Upton, N.  Effects of centrally administered orexin-B and orexin-A; a role for orexin-1 receptors on orexin-B-induced hyperactivity. Psychopharmacology, 2001, 153, 210-218.
  28. Bingham, S.; Davey, P. T.; Babbs, A. J.; Irving, E. A.; Sammons, M. J.; Wyles, M.; Jeffrey, P.; Cutler, L.; Riba, I.; Johns, A.; Porter, R. A.; Upton, N.; Hunter, A. J.; Parsons, A. A.  Orexin-A, an hypothalamic peptide with analgesic properties.    Pain  2001,  92(1-2),  81-90.
  29. Khan, Afzal; Marson, Charles M.; Porter, Rod A..  Synthesis of exocyclic enamides via stereocontrolled allylic isomerization and 1,3-transposition.    Synthetic Communications  2001,  31(11),  1753-1764
  30. Gallagher, T.; Pardoe, D. A.; Porter, R. A.  Synthesis of substituted 2-mercaptobenzaldehydes and 2-substituted benzo[b]thiophenes.    Tetrahedron Lett.  (2000),  41(28),  5415-5418.
  31. Haynes, A. C.; Jackson, B.; Chapman, H.; Tadayyon, M.; Johns, A.; Porter, R. A.; Arch, J. R. S.  A selective orexin-1 receptor antagonist reduces food consumption in male and female rats.    Regul. Pept.  (2000),  96(1-2),  45-51.
  32. Helen F. Boyd, Stephen C. M. Fell, Sean T. Flynn, Deirdre M. B. Hickey, Robert J. Ife, Colin A. Leach, Colin H. Macphee, Kevin J. Milliner, Kitty E. Moores, Ivan L. Pinto, Rod A. Porter, D. Anthony Rawlings, Stephen A. Smith, Ian G. Stansfield, David G. Tew, Colin J. Theobald and Caroline M. Whittaker, N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A2,  Bioorg. Med. Chem. Letters, 2000, 10, 2557
  33. Smart, D.; Jerman, J. C.; Brough, S. J.; Neville, W. A.; Jewitt, F.; Porter, R. A.. The hypocretins are weak agonists at recombinant human orexin-1 and orexin-2 receptors. Br. J. Pharmacol. (2000), 129(7), 1289-1291
  34. Hagan, Jim J.; Leslie, Ron A.; Patel, Sara; Evans, Martyn L.; Wattam, Trevor A.; Holmes, Steve; Benham, Christopher D.; Taylor, Stephen G.; Routledge, Carol; Hemmati, Panida; Munton, Richard P.; Ashmeade, Tracey E.; Shah, Ajit S.; Hatcher, Jonathan P.; Hatcher, Paula D.; Jones, Declan N. C.; Smith, Martin I.; Piper, David C.; Hunter, A. Jackie; Porter, Rod A.; Upton, Neil.  Orexin A activates locus coeruleus cell firing and increases arousal in the rat.    Proc. Natl. Acad. Sci. U. S. A.  (1999),  96(19),  10911-10916
  35. Brown AM, Avenell K, Young TJ, Ho M, Porter RA, Vimal M, et al. (1997). BRL 54443, a potent agonist with selectivity for human cloned 5-ht1E and 5-ht1F receptors. Br J Pharmacol 123: 233
  36. Hursthouse, Michael B.; Khan, Afzal; Marson, Charles M.; Porter, Rod A..  Tin(IV)-mediated stereoselective synthesis of epoxides with concomitant alkyl peroxide formation.    Tetrahedron Lett.  (1995),  36(33),  5979-82.
  37. Page, Philip C. Bulman; Gareh, M. Thomas; Porter, Roderick A..  N-Acylimidazoles: excellent acyl electrophiles for 1,3-dithiane oxide anions.    Tetrahedron Lett.  (1993),  34(32),  5159-62.
  38. Page, Philip C. Bulman; Gareh, M. Thomas; Porter, Roderick A..  Asymmetric oxidation of dithiane derivatives: enantiomerically pure 1,3-dithiane 1-oxide.    Tetrahedron:  Asymmetry  (1993),  4(10),  2139-42.
  39. Booth, R. F. G.; Manley, P. W.; Buckham, S. P.; Hassall, D. G.; Honey, A. C.; Lad, N.; Lunt, D. O.; Oswald, S.; Porter, R. A.; Tuffin, D. P.  5-[6-1-(Cyclohexyl-1H-tetrazol-5-yl)hexyl]-1,8-naphthyridin-2-(1H)-one, SC-44368, a potent anti-aggregatory agent which selectively inhibits platelet cyclic AMP phosphodiesterase.    Platelets  (1992),  3(3),  129-36.
  40. Page, Philip C. Bulman; Jennens, David C.; Porter, Roderick A.; Baldock, Alan N.  A model for the synthesis of the tigliane and daphnane diterpenes using an intramolecular Diels-Alder reaction.  Synlett  (1991),   (7),  472-4.
  41. Manley, Paul W.; Tuffin, David P.; Allanson, Nigel M.; Buckle, Philip E.; Lad, Nagin; Lai, Steve M. F.; Lunt, David O.; Porter, Roderick A.; Wade, Patricia J.  Thromboxane synthase inhibitors.  Synthesis and pharmacological activity of (R)-, (S)-, and ()-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)methoxy]methyl]ethoxy]hexanoic acids.    J. Med. Chem.  (1987),  30(10),  1812-18.
  42. Booth, Robert F. G.; Buckham, Susan P.; Lunt, David O.; Manley, Paul W.; Porter, Roderick A..  Dibenzoquinazolinediones as antihypertensive cyclic guanosine monophosphate phosphodiesterase inhibitors.    Biochem. Pharmacol.  (1987),  36(20),  3517-21.
  43. De Laszlo, Stephen E.; Ley, Steven V.; Porter, Roderick A..  Synthetic approaches to the teleocidin-related tumor promoters: a total synthesis of ()-indolactam V.    J. Chem. Soc., Chem. Commun.  (1986),   (4),  344-6.
  44. Goodchild, John; Porter, Roderick A.; Raper, Robert H.; Sim, Iain S.; Upton, Roger M.; Viney, Julie; Wadsworth, Harry J.  Structural requirements of olefinic 5-substituted deoxyuridines for antiherpes activity.    J. Med. Chem.  (1983),  26(9),  1252-7.
  45. Sim, Iain S.; Goodchild, John; Meredith, David M.; Porter, Roderick A.; Raper, Robert H.; Viney, Julie; Wadsworth, Harry J.  Possible molecular basis for antiviral activity of certain 5-substituted deoxyuridines.    Antimicrob. Agents Chemother.  (1983), 23(3),  416-21.
  46. Ley, S. V.; Porter, R. A.; Gordon, P. F.; Nelson, A. J.  Organometallics in synthesis.    Gen. Synth. Methods  (1983), 6  218-76.
  47. Goodchild, John; Porter, Roderick A.; Raper, Robert H.; Sim, Iain S.; Upton, Roger M.; Viney, Julie; Wadsworth, Harry J.  Structural requirements of olefinic 5-substituted deoxyuridines for antiherpes activity.    J. Med. Chem.  (1983),  26(9),  1252-7.
  48. Ley, Steven V.; Porter, Roderick A..  An unexpected rearrangement of 4-alkylaminoindoles.  J. Chem. Soc., Chem. Commun.  (1982),   (23),  1356-7.
  49. Markham, A. F.; Newton, C. R.; Porter, R. A.; Sim, I. S.  Synthesis of some 5′-amino-2′,5′-dideoxy-5-iodouridine derivatives and their antiviral properties against herpes simplex virus.    Antiviral Res.  (1982),  2(6),  319-30.
  50. Ley, S. V.; Porter, R. A.; Gordon, P. F.; Nelson, A. J.  Organometallics in synthesis.    Gen. Synth. Methods  (1982),  5  208-56.
  51. Markham, A. F.; Porter, R. A.; Gait, M. J.; Sheppard, R. C.; Kerr, I. M.  Rapid chemical synthesis and circular dichroism properties of some 2′-5′-linked oligoriboadenylates.    Nucleic Acids Res.  (1979),  6(7),  2569-82.