Publications for Timothy J. Hagen (>2100 citations; H-index=24):

  1. “Chirality and Drug Discovery” Timothy J. Hagen, Travis R. Helgren Burger's Medicinal Chemistry and Drug Discovery, D.J. Abraham (Ed.). (2020) in press
  2. “Antibacterial activity of 2-amino-4-hydroxypyrimidine-5-carboxylates and binding to Burkholderia pseudomallei 2-C-methyl-D-erythritol-2,4-cyclodiphosphate synthase” Watkins, Sydney M.; Ghose, Debarati; Blain, Joy M.; Grote, Dakota L.; Luan, Chi-Hao; Clare, Michael; Meganathan,R.; Horn, James R.; Hagen, Timothy J. Bioorganic & Medicinal Chemistry Letters (2019), 29(20), 126660. DOI:10.1016/j.bmcl.2019.126660
  3. “Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for Treatment of Fragile X Syndrome and Other Brain Disorders” Mark E. Gurney, Richard A. Nugent, Xuesheng Mo, Janice A. Sindac, Timothy J. Hagen, David Fox III, James M. O’Donnell, Chong Zhang, Ying Xu, Han-Ting Zhang, Vincent E. Groppi, Marc Bailie, Ronald E. White, Donna L. Romero, A. Samuel Vellekoop, Joel R. Walker, Matthew D. Surman, Lei Zhu, Robert F. Campbell Med. Chem., 2019;62(10):4884-4901. doi: 10.1021/acs.jmedchem.9b00193.
  4. Dissemination of Imidacloprid Through Dairy Cattle Manure and Its Effect on the Biological Control Agent, Spalangia endius (Hymenoptera: Pteromalidae), and a Filth Fly Host, Musca domestica (Diptera: Muscidae) Edwin R Burgess, IV Sydney M Watkins  Bethia H King  Karley Chantos-Davidson Aspen N Kremer  Jennifer C Tournear  Joseph Morrow  Timothy J Hagen Elizabeth R Gaillard J Econ Entomol. 2019;112(2):974-980. doi: 10.1093/jee/toy386.
  5. Compound D159687, a phosphodiesterase 4D inhibitor, induces weight and fat mass loss in aged mice without changing lean mass, physical and cognitive function” Muo, Ijeoma M.; Park, Sung-Jun; Smith, Antoine; Springer, Danielle A.; Allen, Michele D.;Hagen, Timothy J.; Chung, Jay H. Biochemical and Biophysical Research Communications 2018,506(4),1059-1064 DOI: 10.1016/j.bbrc.2018.10.180
  6. “The Identification of Inhibitory Compounds of Rickettsia prowazekii Methionine Aminopeptidase for Antibacterial Applications”  Travis R Helgren, Elif S Seven, Congling Chen, Thomas E Edwards, Bart L Staker, Jan Abendroth, Peter J Myler, James R Horn, Timothy Hagen, Med.Chem. Lett 2018, 28(8),1376-1380.  doi: 10.1016/j.bmcl.2018.03.002
  7. “(Z)-4-Chloro-N-{3-[(4-chlorophenyl)sulfonyl]-2,3-dihydrobenzo[d]thiazol-2-ylidene}benzenesulfonamide” Watkins SM, Hagen TJ, Perkins TS, Zheng C. 2017:Ahead of Print. doi: 10.1107/s2414314617008653.
  8. Helgren TR, Hagen TJ. Demonstration of AutoDock as an Educational Tool for Drug Discovery. J Chem Educ. 2017;94(3):345-9. doi: 10.1021/acs.jchemed.6b00555.
  9. Helgren TR, Chen C, Wangtrakuldee P, Edwards TE, Staker BL, Abendroth J, Sankaran B, Housley NA, Myler PJ, Audia JP, Horn JR, Hagen TJ. Rickettsia prowazekii methionine aminopeptidase as a promising target for the development of antibacterial agents. Bioorg Med Chem. 2017;25(3):813-24. doi: 10.1016/j.bmc.2016.11.013.
  10. “Advances in Bacterial Methionine Aminopeptidase Inhibition” Helgren TR, Wangtrakuldee P, Staker BL, Hagen TJ. Curr Top Med Chem (Sharjah, United Arab Emirates). 2016;16(4):397-414. doi: 10.2174/1568026615666150813145410.
  11. “Phthalazines” Timothy J. Hagen and Travis R. Helgren, Science of Synthesis Knowledge update Thieme 2015 137-172.
  12. ”Synthesis and biological evaluation of pyrazolopyrimidines as potential antibacterial agents.” Gashaw M. Goshu, Debarati Ghose, Joy M. Bain, Phillip G. Pierce, Darren W. Begley, Stephen N. Hewitt, Hannah S. Udell, Peter J. Myler, R. Meganathan, Timothy J. Hagen. Med.Chem. Lett 2015 25(24), 5699-5704. DOI: 10.1016/j.bmcl.2015.10.096
  13. “The synthesis, antimalarial activity and CoMFA analysis of novel aminoalkylated quercetin analogs” Helgren, Travis R.; Sciotti, Richard J.; Lee, Patricia; Duffy, Sandra; Avery, Vicky M.; Igbinoba, Osayawemwen; Akoto, Matthew; Hagen, Timothy J. Bioorganic & Medicinal Chemistry Letters 2015, 25(2), 327-332.
  14. “Discovery of triazines as selective PDE4B versus PDE4D inhibitors” Hagen, Timothy J.; Mo, Xuesheng; Burgin, Alex B.; Fox, David; Zhang, Zheng; Gurney, Mark E. Bioorganic & Medicinal Chemistry Letters 2014, 24(16), 4031-4034. DOI: 10.1016/j.bmcl.2014.06.002
  15. “Cytidine derivatives as IspF inhibitors of Burkolderia pseudomallei.” “Zhang, Z.; Jakkaraju, S.; Blain, J.; Gogol, K.; Zhao, L.; Hartley, R. C.; Karlsson, C. A.; Staker, B. L.; Edwards, T. E.; Stewart, L. J.; Myler, P. J.; Clare, M.; Begley, D. W.; Horn, J. R.; Hagen, T. J., Med. Chem. Lett. 2013, 23, 6860-6863.
  16. “Discovery of inhibitors of Burkholderia pseudomallei methionine aminopeptidase with antibacterial activity.” Wangtrakuldee, M.S. Byrd, C.G. Campos, M.W. Henderson, Z. Zhang, A. Masoudi, P.J. Myler, J.R. Horn, P.A. Cotter, T.J. Hagen 2013, ACS Med. Chem. Lett. 2013, 699-703. doi: 10.1021/ml400034m
  17. “A concise synthesis of biaryl PDE4D allosteric modulators.” Dalby, A.; Mo, X.; Stoa, R.; Wroblewski, N.; Zhang, Z.; Hagen, T. J., Tetrahedron Lett. 2013, 54 2737-2739.
  18. “Triazoles and Tetrazoles” T.J. Hagen and Z. Zhang, Heterocyclic Chemistry in Drug Discovery , Ed. by Jie Jack Li, John Wiley & Sons, 2013, 373-397, ISBN-13: 9781118148907
  19. “Recent Trends in Biomarker Research and Development” T.J. Hagen Biochem Anal Biochem 2012, 1:4 1-3.
  20. “1,2-diselenins”, Hagen, T.J., Science of Synthesis2011, 16, 93-97.
  21. “1,4-diselenins”, Hagen, T.J., Science of Synthesis 2011, 16, 99-102.
  22. “Optimization of a Pd-catalyzed intramolecular a-arylation synthesis of tricyclo-[,7]-trideca-2,4,6-trien-13-ones.” Powell, N.A.; Hagen, T.J.; Ciske, F.L.; Cai, C.; Duran, J.E.; Holsworth, D.D.; Leonard, D.; Kennedy, R.M.; Edmunds, J.J. Lett. 2010 51: 4441-4444.
  23. “Design of phosphodiesterase 4D (PDE4D) allosteric modulators for enhancing cognition with improved safety.” Burgin, A.B.; Magnusson, O.T.; Singh, J.; Witte, P.; Staker, B.L.; Bjornsson, J.M.; Thorsteinsdottir, M.; Hrafnsdottir, S.; Hagen, T.J.; Kiselyov, A.S.; et al Nature Biotechnology, 2010 28(1), 63-70.
  24. “Chirality and Biological Activity” Jasbir Singh and Timothy J. Hagen, Burger's Medicinal Chemistry and Drug Discovery, Volume 7, Ed by Donald J. Abraham, John Wiley & Sons, 2010, 127-166.
  25. “The Barton Nitrite Photolysis” Hagen, Timothy J; Name Reactions for Chain Extension, Ed. by Jie Jack Li, John Wiley & Sons, 2009, 633-647.
  26. “The Zaitsev Elimination” Hagen, Timothy J; Name Reactions for Functional Group Transformations, Ed. by Jie Jack Li and E. J. Corey, John Wiley & Sons, 2007, 414-421.
  27. “The Prilezhaev Reaction”, Hagen, Timothy J; Name Reactions for Functional Group Transformations, Ed. by Jie Jack Li and E. J. Corey, John Wiley & Sons, 2007, 274-281.
  28. “5-Fluorinated L-Lysine Analogues as Selective Induced Nitric Oxide Synthase Inhibitors.”      Hallinan, E. Ann; Hagen, Timothy J.; Bergmanis, Arija; Moore, William M.; Jerome, Gina M.; Spangler, Dale P.; Stevens, Anna M.; Shieh, Huey S.; Manning, Pamela T.; Pitzele, Barnett S.    Med. Chem. 2004,  47(4),  900-906.
  29. “3-Hydroxy-4-methyl-5-pentyl-2-iminopyrrolidine: A potent and highly selective inducible nitric oxide synthase inhibitor.” Tsymbalov, Sofya; Hagen, Timothy J.; Moore, William M.; Jerome, Gina M.; Connor, Jane R.; Manning, Pamela T.; Pitzele, Barnett S.; Hallinan, E. Ann. & Med. Chem.  Lett. 2002 12(22), 3337-3339. 
  30. “Syntheses of new conformationally constrained S-[2-[(1-iminoethyl)amino]ethyl]homocysteine derivatives as potential nitric oxide synthase inhibitors.” Wang, Lijuan J.; Grapperhaus, Margaret L.; Pitzele, Barnett S.; Hagen, Timothy J.; Fok, Kam F.; Scholten, Jeffrey A.; Spangler, Dale P.; Toth, Mihaly V.; Jerome, Gina M.; Moore, William M.; Manning, Pamela T.; Sikorski, James A. Chem. 2002, 13(1), 77-83. 
  31. “2,4-Disubstituted Oxazoles and Thiazoles as Latent Pharmacophores for Diacylhydrazine of SC-51089, a Potent PGE2” Hallinan, E.A.; Hagen, T.J.; Tsymbalov, S.; Husa, Staplefeld, A.; Savage, M.A. Biorgan. and Med. Chem., 2001, 1-6.
  32. "Specific Inhibitors of Inducible Nitric Oxide Synthase: Efficacy in a Rodent Model of Sepsis." Fretland, D.J.; Widomski, D.L.; Anglin, C.P.; Moore, W.M.; Jerome, G.; Kornmeier, C.; Connor, J.; Branson, L.; Wyatt, P.; Manning, P.; Toth, M.; Webber, R.K.; Hansen, D.W.;  Hallinan, E.A.; Hagen, T.J.; Bergmanis, A.; Pitzele, B.;  and Currie, M.G.; Res. 48. Supplement 2 1999, 796-797.
  33. “2-Iminopyrrolidines as Potent and Selective Inhibitors of Human Inducible Nitric Oxide Synthase.” Hagen, T.J.; Bergmanis, A.A.; Kramer, S.W.; Fok, K.F.; Schmelzer, A.E.; Pitzele, B.S.; Swenton, L.; Jerome, G.M.; Kornmeier, C.M.; Moore, W.M.; Connor, J.R.; Branson, L.F.; Manning, P.T.; Currie, M.G. and Hallinan, E.A. Med. Chem. 1998, 41, 3675-3683.
  34. “Substituted 2-Iminopiperidines as Inhibitors of Human Nitric Oxide Synthase Isoforms.” Webber, R.K.; Metz, S.; Moore, W.M.; Connor, J.R.; Currie, M.G.; Fok, K.F.; Hagen, T.J.; Hansen, Jr., D.W.; Jerome, G.M.; Manning, P.T.; Pitzele,B.S.; Toth, M.V.; Trivedi, M.; Zupec, M.E.; Tjoeng, F. S. Med. Chem. 1998, 41, 96-101.
  35. “Aminoacetyl Moiety as a Potential Surrogate for Diacylhydrazine Group of SC-51089, a Potent PGE2Antagonist, and Its Analogs.” Hallinan, E.A.; Hagen, T.J.; Tsymbalov, S.; Husa, R.K.; Lee, A.C.; Stapelfeld, A.; Savage, M.A. Med. Chem. 1996, 39, 609-613.
  36. “Structure-activity Relationships in Antagonist and Inverse Agonist ligands for the Benzodiazepine Receptor.” Codding, P.W.; Roszak, A.W.; Szkaradzinska, M.B.; Cook, J.M.; Hagen, T.J.; Allen, M.S. J. Chem. 1995, 73, 499-512.
  37. “BZ1Receptor Selective Specific Ligands. Synthesis and Biological Properties of BCCt, a BZ1 Receptor Subtype Specific Antagonist.” Cox, E.D.; Hagen, T.J.; McKernan, R.M.;  Cook, J.M. Chem. Res. 1995, 5, 710-718.
  38. “Lithiation and Electrophilic Substitution of 8-Chlorodibenz[b,f][1,4]-oxaze[ine-10-tertbuty]carbamate: The preparation of Novel Fused Heterocyclic Derivatives of 8-Chlorodibenzoxazepine.” Li, J.J.; Hagen, T.J.; Chrusciel, R.A.; Norton, M.B.; Tsymbalov, S.; Hallinan, E.A.; Reitz, D.B. Heterocyclic. Chem., 31, 1994,1689-96.
  39. “The N-Boc Group as an Activator for the a-Lithiation of Carbamates: Synthesis of 11-Substituted Dibenzoxazepines.”  Hagen, T.J.; Rafferty, M.F.; Collins, J.T.; Garland, D.J.; Li, J.J.; Norton, M.B.; Reitz, D.B.; Tsymbalov, S.; Pitzele, B.S.; Hallinan, E.A. Heterocycles 1994, 38, 601-611.
  40. “N-Substituted Dibenzoxazepines as analgesic PGE2” Hallinan, E.A.; Hagen, T.J.; Husa, R.K.; Tsymbalov, S.; Rao, S.N.; vanHoeck, J.P.; Rafferty, M.F.; Stapelfeld, A.; Savage, M.A.; Reichman, M. J. Med. Chem. 1993, 36, 3293-9.
  41. “Predictive Binding of b-Carboline Inverse Agonists and Antagonists via the CoMFA Approach.” Allen, M.S.; LaLoggia, J.; Dorn, L.J.; Martin, M.J.; Constantino, G.; Hagen, T.J.; Koehler, K.F.; Skolnick, P.; Cook, J.M. Med. Chem.  1992, 35, 4001-10.
  42. “Synthetic and Computer Assisted Analysis of the Pharmacophore for Agonists at Benzodiazepine Receptors.” Diaz-Arauzo,H; Koehler, K.F.; Hagen, T.J.; Cook, J.M.  Life Sci. 1991, 49, 207-16.
  43. “Synthetic and Computer Assisted Approaches to the Pharmacophore of the Benzodiazepine Receptor Inverse Agonist Site.” Allen, M.S.; Yun-C,T.; Trudell, M.L.; Narayanan, K.; Schindler, L.R.; Martin, M.; Hagen, T.J.; Koehler, K.F.; Codding, P.W.; Skolnick, P.;Cook, J.M. Med. Chem. 1990, 33, 2343-57.
  44. “Regioselective Functionalization of Medium Ring Lactams.” Hagen, T.J. Synlett 1990, 1, 63.
  45. “DDQ Oxidations in the Indole Area; The Total Synthesis of 1-Methoxycanthin-6-one and an Improved Synthesis of Crenatine.” Hagen, T.J.; Narayanan, K.; Cook, J.M. Org. Chem. 1989, 54, 2170-8.
  46. “Inhibition of Sleep and Benzodiazepine Receptor Binding by a b-Carboline Derivative.” Martin, J.J.; Cook, J.M.; Hagen, T.J.; Mendelson, W.B. Biochem. Behav. 1989, 34, 37-42.
  47. “Behaviorial effects of benzodiazepine antagonists in chlordiazepoxide tolerant and non-tolerant rats.” Takada,K.; Suzuki, T.; Hagen, T.; Cook, J.M.; Katz, J.L. Life Sci. 1989, 44,  289-99.
  48. “Structure-activity Studies of b-Carbolines. Crystal and molecular structures of t-butyl b-carboline-3-carboxylate and  2-(methoxycarbonyl)canthin-6-one. Codding, P.; Szkaradzinska, M.B.; Roszak, A.; Hagen, T.J.; Cook, J.M. Can. J. Chem. 1988,66(12), 2981.
  49. “3-Ethoxy-b-Carboline: A High Affinity Benzodiazepine Receptor Ligand with Partial Inverse Agonist Properties.” Trullas, R.; Ginter, H.; Jackson, B.; Skolnick, P.; Allen, M.; Hagen, T.; Cook, J.M. Life Sci.  1988, 43, 1189-97.
  50. “Synthesis of 1-Methoxycanthin-6-one.” Hagen T.J.; Cook, J.M. Tetrahedron Lett. 1988, 29, 2421-4.
  51. “b-Carbolines as Antagonists of the Discriminative Stimulus Effects of Diazepam in Rats.” Shannon, H.E.; Hagen, T.J.; Guzman, F.; Cook, J.M. Pharm. Exp. Ther. 1988, 246, 275-81.
  52. “Synthesis of Novel 3-Substituted b -Carbolines as Benzodiazepine Receptor Ligands: Probing the Benzodiazepine Receptor Pharmacophore.” Cook, J.M.; Allen, M.S.; Hagen, T.J.; Trudell, M.L.; Codding, P.; Skolnick, P. Med. Chem. 1988, 31, 1854-61.
  53. “Discriminative Stimulus Effects of Intravenous Nicotine in Squirrel Monkeys.” Takada, K.; Hagen, T.J.; Cook, J.M.; Goldberg, S.A.; Katz, J.L. Biochem. Behav. 1988, 30, 243-7.
  54. “Synthesis of 6-substituted b-Carbolines That Behave as Benzodiazepine Receptor Antagonists an Inverse Agonists.” Hagen, T.J.; Skolnick, P.; Cook, J.M. Med. Chem. 1987, 30,750-3.
  55. “Synthesis of 3,6-Disubstituted b -Carbolines Which Possess Either Benzodiazepine Antagonist or Agonist Activity.” Hagen, T.J.; Guzman, F.; Schultz, C.; Skolnick, P.; Cook, J.M. Heterocycles 1986, 24, 2845-55.
  56. “Cerebrovascular and Cerebral Metabolic Effects of Physostigmine, Midazolam, and a Benzodiazepine Agonist.” Hoffman, W.E.; Albrecht, R.F.; Miletich, D.J.; Hagen, T.J.; Cook J.M. Analg. 1986, 65, 639-44.
  57. “Biomimetic Approach to Potential Benzodiazepine Agonists and ” Guzman, F.; Cain,M.; Larschied, P.; Hagen, T.J.; Cook, J.M.; Schweri, M.; Skolnick, P.; Paul, S.M. J. Med. Chem. 1984, 27, 564-70.
  58. “Photochemical Aromatic Cyanomethylation: Aromatic substitution by way of radical cations.” Kurz, M.E.; Lapin, S.C.; Miriam, K.; Hagen T.J.; Qain, X.Q. Org. Chem. 1984,49, 2728-33. 

Contact Us

Faraday Hall 350
Northern Illinois University
DeKalb, IL 60115

Phone: 815-753-1463
Fax: 815-753-2902

Mailing Address

Timothy J. Hagen, Ph.D.
Department of Chemistry and Biochemistry
Northern Illinois University
1425 W. Lincoln Hwy.
DeKalb, IL 60115‐2828
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