PUBLICATIONS

  1. Knutsen, L.J.S.; Aimone, L.D.; Bacon, E.R.; Lyons, J.; Prouty, C.P.; Raddatz, R.; Sundar, B. and Hudkins, R.L. 3,6-Disubstituted Pyridazines as Novel Analogues of CEP-26401: CNS Penetrant Histamine H3 Receptor Antagonists. Med. Chem. Lett., manuscript submitted.
  2. Hudkins, R.L.; Raddatz, R.; Tao, M.; Mathiasen, J.R..; Aimone, L.D.; Becknell, N.C.; Prouty, C.P.;. Knutsen, L.J.S.; Yazdanian, M.; Moachon, G.; Ator, M.A.; Mallamo, J.P.; Marino, M.J.; Bacon, E.R. and Williams, M. Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)prop-oxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H3 Receptor Inverse Agonist. Med. Chem., 2011, 54, 4781-4792.
  3. Knutsen, L.J.S. Drug Discovery Management, Small is Still Beautiful; Why Many Companies get it Wrong. Drug Discovery Today, 2011, 16, 476-484.
  4. Gillespie, R.J.; Adams, D.R.; Bebbington, D.; Benwell, K.; Cliffe, I.A.; Dawson C.E.; Dourish, C.T.; Fletcher, A.; Gaur, S; Giles, P.R.; Jordan, A.M.; Knight, A.R.; Knutsen, L.J.S.; Lawrence, A.; Lerpiniere, J.; Misra, A.; Porter, R.H.P.; Pratt, R.M.; Shepherd, R. Upton, R.; Ward, S.E.; Weiss, S.M. and  Williamson. D.S. Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. Bioorg. Med. Chem. Lett., 2008, 18, 2916 – 2919.
  5. Marino, M.J.: Knutsen, L.J.S and Williams M.  Perspective: Emerging Opportunities for Antipsychotic Drug Discovery in the Postgenomic Era J. Med. Chem., 2008, 51, 1077 – 1107.
  6. Knutsen, L.J.S., Hobbs, C.J.; Earnshaw, C.G., Fiumana, A., Gilbert, J., Mellor, S.L., Radford, F., Smith, N.J., Birch, P.J., Burley, R., Thomas, D., Ward, S.D.C. and James, I.F.  Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers. Bioorg. Med. Chem. Lett., 2007, 17, 662 – 667.
  7. Marino, M.J.: Davis, R.E.; Meltzer, H.E.; Knutsen, L.J.S and Williams M. Schizophrenia. In Comprehensive Medicinal Chemistry II (Taylor, J.B; Triggle, D. J., Editors-in-Chief) Vol. 6; Therapeutic Areas I (M. Williams, Volume Editor), 2006, pp. 17 – 44.
  8. Knutsen, L.J.S and Williams M. Epilepsy. In Comprehensive Medicinal Chemistry II (Taylor, J.B; Triggle, D. J., Editors-in-Chief) Vol. 6; Therapeutic Areas I (M. Williams, Volume Editor), 2006, pp 279 – 296.
  9. Bowdle, T. A., Knutsen, L.J.S and Williams M. Local and Adjunct Anesthesia. In Comprehensive Medicinal Chemistry II (Taylor, J.B; Triggle, D. J., Editors-in-Chief) Vol. 6; Therapeutic Areas I (M. Williams, Volume Editor), 2006, pp 351 – 368.
  10. Haldeman, M.; Vieira, B.; Winer, F. and Knutsen, L.J.S.  Exploration Tools for Drug Discovery and Beyond: Applying SciFinder® to Interdisciplinary Research. Current Drug Discovery Technologies, 2005, 2, 69 – 74.
  11. Knutsen, L.J.S.; Weiss, S.M; KW-6002, Kyowa Hakko Kogyo. Curr. Opin. Invest. Drugs (PharmaPress Ltd.), 2001, 2, 668 – 673.
  12. Jacobson, K.A. and Knutsen, L.J.S.; P1 and P2 Purine and Pyrimidine Receptor Ligands.  In Handbook of Experimental Pharmacology, Volume 151/I: Purinergic and Pyrimidinergic Signalling I; Abbracchio M.P. and Williams, M., Eds.; Springer-Verlag: Berlin, Germany; 2001, pp 129 – 175.
  13. Bentley, J.M., Cliffe, I.A., Knutsen, L.J.S., Monck, N.J. Medicinal Chemistry – 1 International Symposium, I Drugs, 2000, 3, 1457 – 1486.
  14. Dhanda, A.; Knutsen, L.J.S.; Nielsen, M-B; Roberts, S.M.; Varley, D.R.  Facile conversion of 4-endo-hydroxy-2-oxabicyclo[3.3.0]oct-7-en-3-one into carbocyclic 2′-deoxyribonucleoside analogues.  J. Chem. Soc., Perkin Trans. 1, 1999, 23, 3469 – 3475.
  15. Cliffe, I.A., Bebbington, D., Gillespie, R.J. and Knutsen, L.J.S. RSC-SCI Tenth Medicinal Chemistry Symposium, I Drugs, 1999, Week 38, 25 – 29.
  16. Andersen, K.E; Sorensen, J.L.; Huusfeldt, PO.; Knutsen, L.J.S.; Lau, J.; Lundt, B.F.; Petersen, H.; Suzdak, P.D.; Swedberg, M.D.B. Synthesis of Novel GABA Uptake Inhibitors. 4. Bioisosteric Transformation and Successive Optimization of Known GABA Uptake Inhibitors Leading to a Series of Potent Anticonvulsant Drug Candidates. J. Med. Chem., 1999, 42, 4281 – 4291.
  17. Knutsen, L.J.S., Lau, J., Petersen, H., Thomsen, C., Weis, J.U., Shalmi, M., Judge, M.E., Hansen, A.J. and Sheardown, M.J.; N-Substituted Adenosines as Novel Neuroprotective A1 Agonists with Diminished Hypotensive Effects. J. Med. Chem., 1999, 42, 3463 – 3477.
  18. Knutsen, L.J.S., Andersen, K.E., Lau, J., Lundt, B.F., Henry, R.F., Morton, H.E., Nærum, L., Petersen, H., Stephensen, H., Suzdak, P.D., Swedberg, M.D.B., Thomsen, C. and Sørensen P.O. The Synthesis of Novel GABA Uptake Inhibitors. 3. Diaryloxime and Diarylvinylether Derivatives of Nipecotic acid and Guvacine as Anticonvulsant Agents.  J. Med. Chem., 1999, 42, 3447 – 3462.
  19. Knutsen L.J.S., Sheardown M.J., Roberts S.M., Mogensen J.P., Olsen U.B., Thomsen, C. and Bowler A.N.  Adenosine A1 and A3 Selective N-Alkoxypurines as novel Cytokine Modulators and Neuroprotectants Drug Dev. Res. 1998, 45, 214 – 221.
  20. Mogensen, J.P., Roberts, S.M., Bowler, A.N., Thomsen, C. and Knutsen, L.J.S.; The Synthesis of New Adenosine A3 Selective Ligands Containing Bioisosteric Isoxazoles. Bioorg. Med. Chem. Lett. 1998, 8, 1767 – 1770.
  21. Barkley, J.V., Dhanda, A., Knutsen, L.J.S., Nielsen, M-B., Roberts, S.M. and Varley, D.R. Stereoselective Conversion of 2′,3′-Dideoxydidehydrocarbocyclic nucleosides into 2′-Deoxycarbocyclic nucleosides. Chem. Commun. 1998, 1117 – 1118.
  22. Thomsen, C., Valsborg, J.S., Foged, C. Knutsen, L.J.S. Characterization of [3H]-N-[R-(2-benzothiazolyl)thio-2-propyl]-2-chloroadenosine ([3H]-NNC 21-0136) binding to rat brain: profile of novel selective agonist for adenosine A1 receptors. Drug Dev. Res. 1997, 42, 86 – 97.
  23. Knutsen, L.J.S. and Murray, T.F. Adenosine and ATP in Epilepsy. Purinergic Approaches Exp. Ther. (1997), 423 – 447.  Editors: Jacobson, Ken A.; Jarvis, Michael F.  Publisher: Wiley-Liss, New York, N. Y.
  24. Sheardown, M.J. and Knutsen, L.J.S.; Unexpected Neuroprotection Observed with the Adenosine A2A Receptor Agonist CGS 21680. Drug Dev. Res., 1996, 39, 108 – 114.
  25. Valsborg, J.S., Knutsen, L.J.S., and Foged, C.; 14C-labelling of a Novel Antiischaemic Adenosine A1 Agonist at purine C-8. J. Labelled Compounds Radiopharm., 1996, 38, 497 – 507.
  26. Sheardown, M.J., Hansen A.J., Thomsen, C., Judge, M.E. and Knutsen, L.J.S.; Novel Adenosine Agonists: A Strategy for Stroke Therapy. In Ischemic Stroke: Recent Advances in Understanding and Therapy: Grotta, J., Miller, L., Buchan, A.M., Eds.; Published by International Business Communications, 1995, pp 187 – 214.
  27. Hibbs, D.E., Hursthouse, M.B., Knutsen, L.J.S., Abdul Malik, K.M., Olivio, H.F., Roberts, S.M., Sik, V.M., Varley, D.R. and Xiong, H.; Preparation and Determination of the Absolute Configuration of Optically Active 9-Hydroxy-7-oxabicyclo[4.3.0]non-4-en-8-ones; Acta. Chem. Scand. 1995, 49, 122 – 127.
  28. Valsborg, J.S., Knutsen, L.J.S., Lundt, I and Foged, C.; Synthesis of [8-14C]-2,6-dichloro-9H-purine, a radiolabelled precursor for 14C-nucleosides; J. Labelled Compounds Radiopharm., 1995, 36, 454 – 464.
  29. Knutsen, L.J.S., Lau, J., Eskesen, K., Sheardown, M.J., Thomsen, C., Weis, J.U., Judge, M.E. and  Klitgaard, H.; Anticonvulsant Actions of Novel and Reference Adenosine Agonists. In Adenosine and Adenine Nucleotides: From Molecular Biology to Integrative Physiology; Belardinelli, L. and Pelleg, A., Eds.; Kluwer Academic Publishers: Norwell, MA USA; 1995, pp 479 – 487.
  30. Knutsen, L.J.S., Lau, J., Sheardown, M.J., Thomsen, C.; The synthesis and biochemical evaluation of new A1 selective adenosine receptor agonists containing a 6‑hydrazinopurine moiety; Bioorg. Med. Chem. Lett., 1993, 3, 2661 ‑ 2666.
  31. Klitgaard, H., Knutsen, L.J.S. and Thomsen, C.; Contrasting effects of adenosine A1 and A2 receptor ligands in different chemoconvulsive models; Eur. J. Pharmacol., 1993, 224, 221 ‑ 228.
  32. Andersen, K.E., Braestrup, C., Grønwald, F.C., Jørgensen, A.S., Nielsen, E.B., Sonnewald, U. Sørensen P.O., Suzdak,  P.D. and Knutsen, L.J.S.; The Synthesis of Novel GABA uptake inhibitors. 1. Elucidation of the structure activity studies leading to the choice of R‑1‑[4,4‑bis (3‑methyl‑2‑thienyl)‑3‑but­enyl]‑3‑piper­idine carboxylic acid (Tiagabine) as an anticonvulsant drug candidate; J. Med. Chem., 1993, 36, 1716 ‑ 1725.
  33. Suzdak, P.D.; Frederiksen, K.; Andersen, K.E.; Soerensen, P.O.; Knutsen, L..J.S.; Nielsen, E.B. NNC-711, a novel potent and selective g-aminobutyric acid uptake inhibitor: pharmacological characterization. Eur. J. Pharmacol., 1992, 223, 189 ‑ 198.
  34. Suzdak, P.D., Swedberg, M.D.B., Andersen, K.E., Knutsen, L.J.S. and Braestrup, C.; In vivo labeling of the central GABA Uptake Carrier with 3H‑Tiagabine; Life Sciences, 1992, 51, 1857 ‑ 1868.
  35. Knutsen, L.J.S.; The Chemistry of 2’‑deoxyribo‑C‑nucleosides; Nucleosides Nucleotides, 1992, 11, 961 ‑ 983.
  36. Nielsen, E.B., Suzdak, P.D., Andersen, K.E., Knutsen, L.J.S., Sonnewald, U. and  Braestrup, C.; Characterisation of tiagabine (NO‑328), a new potent and selective GABA‑uptake inhibitor; Eur. J. Pharmacol., 1991, 196, 257 ‑ 266.
  37. Braestrup, C., Nielsen, E.B., Sonnewald, U., Knutsen, L.J.S., Andersen, K.E., Jansen, J.A., Frederiksen, K., Andersen, P.H., Mortensen, A. and Suzdak, P.D.; (R)‑N‑[4,4‑bis­(3‑methyl‑2‑thienyl)‑but‑3‑en‑1‑yl]­nipecotic acid binds with high affinity to the brain g‑aminobutyric acid uptake carrier; J. Neurochem., 1990, 54, 639 ‑ 647.
  38. Braestrup, C., Nielsen, E.B., Wolffbrandt, K.H., Andersen, K.E., Knutsen, L.J.S. and Sonnewald, U.; Modulation of GABA receptor interaction with GABA uptake inhibitors;  Int. Congr. Ser.‑Exerpta Med., 1987, 750 (Pharmacology), 125 ‑ 128.
  39. Mitchell, W.L., Ravenscroft, P., Hill, M.L., Knutsen, L.J.S., Judkins, B.D., Newton, R.F. and Scopes, D.I.C.; Synthesis and antiviral properties of 5‑(2‑substituted-vinyl)‑6‑aza‑2’‑deoxy­uridines; J. Med. Chem., 1986, 29, 809 ‑ 816.
  40. Knutsen, L.J.S., Judkins, B.D., Newton, R.F., Scopes, D.I.C. and Klinkert, G.; Synthesis of imidazo‑fused bridgehead‑nitrogen 2’‑deoxy-ribo‑C‑nucleosides: coupling elimination reactions of 2,5‑anhydro‑ 3,4,6‑tri‑O‑benzoyl‑D‑allonic acid; J. Chem. Soc. Perkin Trans I, 1985, 621 ‑ 630.
  41. Mitchell, W.L., Ravenscroft, P., Hill, M.L., Knutsen, L.J.S., Newton, R.F. and Scopes, D.I.C.; Synthesis and antiviral activity of 5‑halovinyl‑6‑aza‑2’‑deoxyuridines; Nucleosides Nucleotides, 1985, 4, 173 ‑ 175.
  42. Knutsen, L.J.S., Judkins, B.D., Mitchell, W.F., Newton, R.F. and Scopes, D.I.C.; Synthesis of imidazo‑fused bridgehead‑nitrogen C‑nucleo­sides via dehydrative coupling reactions of 2,5‑anhydro‑3,4,6‑tri-O‑­benz­oyl‑D‑allonic acid; J. Chem. Soc. Perkin Trans I, 1984, 229 ‑ 238.
  43. Knutsen, L.J.S., Newton, R.F., Scopes, D.I.C. and Klinkert, G.; Coupling‑elimination reactions of 2,5‑anhydro‑3,4,6‑tri‑O‑benz­oyl‑D‑allonic acid: synthesis of 2’‑deoxy­ribo‑C‑nucleo­sides; Carbohydr. Res., 1982, 110, C5 ‑ C8.
  44. Knutsen, L.J.S., Judkins, B.D., Newton, R.F. and Scopes, D.I.C.; A novel elimination reaction of 3,4,6‑tri‑O‑benzoyl‑2,5‑an­hydro‑D‑allonic acid: ribose to 2’‑deoxyribosyl conversion; Tetrahedron Lett., 1982, 23, 1013 ‑ 1014.

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