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Athens OH 45701
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College of Arts and Sciences
Russ College of Engineering and Technology
Faculty
Stephen Bergmeier, portrait

Stephen C. Bergmeier

Professor
Biomedical Engineering
Chemistry and Biochemistry
Molecular and Cellular Biology
740-597-9649
Chemistry 205, Athens Campus

Education

  • Ph.D., Medicinal Chemistry, University of Michigan, 1990

Research Interests

  • Drug Design
  • Drug Synthesis
  • Pharmaceutical Engineering

Biography

Recent News About Stephen Bergmeier

Research

  • New synthetic methods for the synthesis of heterocyclic rings, Medicinal chemistry - design and synthesis of novel anticancer agents and anti-infective therapies

The synthesis of small and not-so-small organic molecules forms the foundation for our studies in organic chemistry at the interface of chemistry and biology. We view the somewhat disparate research areas of synthetic methodology development and drug discovery as a two-way street. The development of new synthetic methods and new avenues for parallel synthesis provides the inspiration for new directions in drug discovery and development. In a similar fashion, the identification of novel targets for drug discovery can also provide the impetus for the development of new methodology. Our group currently has three ongoing research projects.

Glucose uptake inhibitors as anticancer agents

All cancers rely heavily on glucose as the primary energy source and show increased glucose uptake and glucose metabolism when compared with normal cells. The increased glucose metabolism rates have been associated with hypoxia as well as metastasis and the invasive potential of cancer. Compounds that selectively inhibit basal glucose uptake should be able to inhibit cancer cell growth, induce cancer cell apoptosis, and provide a novel anti-cancer therapeutic strategy. We have designed and prepared novel small molecules that block basal glucose uptake and consequently kill cancer cells. This is a novel mechanism of action for an anticancer drug and the compounds that we have designed are among the most potent glucose uptake inhibitors reported. Our current work in this area is aimed at improving the stability and activity of our lead compounds. Additional ongoing work is focused on determining the SAR of our current lead compounds and understanding the mechanism of action. This work is carried out in collaboration with Prof. X. Chen (Ohio University).

Small molecule modulation of RNA transcription

This project involves the design and synthesis of new molecules that act as antibacterial agents through their specific interactions with the T Box antitermination transcription regulatory element. This work is carried out in collaboration with Prof. J. V. Hines (Ohio University). The initial lead compounds were discovered as part of our earlier research on the development of new chemical reactions. This research project provides an excellent example of how research in synthetic methodology can lead to new drug discovery projects. The oxazolidinones that we prepared were the first molecules to show the ability to modulate the T box antiterminator RNA. Our subsequent work identified additional structural modalities that retain this activity. This work has lead to the identification of the first small molecule modulators of RNA-RNA interactions. Our ongoing research is focused on optimizing the RNA binding and inhibition of the activity of the T Box riboswitch of our initial lead compounds. To that end several conformationally restrained analogs of our initial lead compound are being prepared and studied. Our work is partially guided by molecular modeling and NMR binding studies.

Reactions of aziridines for the synthesis of heterocycles

A key aspect of our research program is the development of new methods and strategies for the synthesis of complex heterocyclic molecules. Many of these methods rely on the formation and reactivity of small strained heterocycles such as aziridines. We have developed a new type of fused ring aziridine which can be used for the preparation of multiple different heterocycles. We have also examined the use of aziridines in ring opening reactions with π-nucleophiles as a route to heteroatom substituted carbocyclic ring systems. Collectively this work provided new methods for the synthesis of heterocycles as well as providing insight into the reactivity of aziridines.

Selected Publications

  • Development of a method for the synthesis of 4-aryl functionalized 2-azabicyclo[3.2.1]octanes. Ian Armstrong, S. C. Bergmeier, Synthesis, 2017, 2733-2742
  • A synthesis of hexahydro H-oxazolo[3,4-a]pyrazin-3-ones from fused aziridines. F. Fang, I. Maciagiewicz, S.C. Bergmeier, Heterocycles 2016, 93, 422-439.
  • Factors that influence T box riboswitch efficacy and tRNA affinity. C. Zeng, S. Zhou, S.C. Bergmeier, J.V. Hines, Bioorg. Med. Chem. 2015, 23, 5702.
  • A small-molecule inhibitor of glucose transporter 1 downregulates glycoloysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo. Y. Liu, Y. Cao, W. Zhang, S. Bergmeier, Y. Qian, H. Akbar, R. Colvin, J. Ding, L. Tong, S. Wu, J. Hines and X. Chen, Mol. Cancer Ther. 2012, 11, 1672-1682.
  • Fused ring aziridines as a facile entry into triazole fused tricyclic and bicyclic heterocycles. F. Fang, M. Vogel, J. V. Hines, S. C. Bergmeier, Org. Biomol. Chem. 2012, 10, 3080-3091.
  • Studies on the ring opening reactions of 3-oxa-1-azabicyclo[3.1.0]hexan-2-ones. Synthesis of aminomethyl oxazolidinones and aziridinyl ureas. S. C. Bergmeier, G. M. Wells, T. Dudding, L. Belding, J. A. Frick, A. Nayek, J. Huang, S. J. Katz, Tetrahedron, 2012, 68, 3980-3987.
  • Small compound inhibitors of basal glucose transport inhibit cell proliferation and induce apoptosis in cancer cells via glucose-deprivation-like mechanisms. Y. Liu, W. Zhang, Y. Cao, Y. Liu, S. C. Bergmeier & X. Chen, Cancer Lett. 2010, 298, 176-185.

Journal Article, Academic Journal (51)

  • Parsons, E., Aldhumani, A., Fairchild, E., Adegbite, O., Roberts, J., Bergmeier, S., Hines, J. (2026). Cyclic Amide-Linked Oxazolidinone Triazoles as Inhibitors of the T-Box Riboswitch . 1. Molecules ; 31: 17. https://doi.org/10.3390/molecules31010029.
  • Parsons, E., Aldhumani, A., Fairchild, E., Adebite, O., Roberts, J., Hines, J., Bergmeier, S. (2025). Cyclic Amide-Linked Oxazolidinone Triazoles as Inhibitors of the T-Box Riboswitch. 1. Molecules; 31.
  • Parsons, E., Aldhumani, A., Fairchild, E., Adegbite, O., Roberts, J., Hines, J., Bergmeier, S. (2025). Cyclic Amide-Linked Oxazolidinone Triazoles as Inhibitors of the T-Box Riboswitch. 1. Molecules; 31: 29. https://doi.org/10.3390/molecules31010029.
  • Ambagaspitiya, T., Garza, D., Skelton, E., Kubacki, E., Knight, A., Bergmeier, S., Cimatu, K. (2025). Using the pH sensitivity of switchable surfactants to understand the role of the alkyl tail conformation and hydrogen bonding at a molecular level in elucidating emulsion stability. Journal of Colloid and Interface Science; 678: 164-175. https://doi.org/10.1016/j.jcis.2024.08.156.
  • Boesger, H., Williams, K., Abdullai, S., Hubble, B., Noori, M., Orac, C., Amesaki, D., Ghazanfari, D., Fairchild, E., Fatunbi, O., Pritchard, J., Goetz, D., Hines, J., Bergmeier, S. (2025). Docking and Structure Activity Relationship Studies of Potent and Selective Thiazolidinethione GSK-3 Inhibitors. Bioorg. Med. Chem. Lett; 117: 130074.
  • Mehrani, R., Mondal, J., Ghazanfari, D., Goetz, D., McCall, K., Bergmeier, S., Sharma, S. (2024). Capturing the Effects of Single Atom Substitutions on the Inhibition Efficiency of Glycogen Synthase Kinase-3β Inhibitors via Markov State Modeling and Experiments. 14. J Chem Theory Comput; 20: 6278-6286.
  • McCall, K., Walter, D., Patton, A., Thuma, J., Courreges de Benencia, M., Palczewski, G., Goetz, D., Bergmeier, S., Schwartz, F. (2023). Anti-Inflammatory and Therapeutic Effects of a Novel Small-Molecule Inhibitor of Inflammation in a Male C57BL/6J Mouse Model of Obesity-Induced NAFLD/MAFLD. 16. Journal of Inflammation Research; 2023: 5339-5366.
  • Ghazanfari, D., Courreges de Benencia, M., Belinski, L., Lloyd, J., Bergmeier, S., McCall, K., Goetz, D. (2022). Mechanistic Insights into SARS-CoV-2 Spike Protein Induction of the Chemokine CXCL10. Submitted.
  • Ghazanfari, D., Courreges, M., Belinski, L., Bergmeier, S., McCall, K., Goetz, D. (2022). Evidence for investigating GSK-3 inhibitors as potential therapeutics for severe COVID-19. Biochemical and Biophysical Research Communications; 605: 171-176.
  • Shriwas, P., Roberts, D., Li, Y., Wang, L., Qian, Y., Bergmeier, S., Hines, J., Adhicary, S., Nielsen, C., Chen, X. (2021). A small-molecule pan-class I glucose transporter inhibitor reduces cancer cell proliferation in vitro and tumor growth in vivo by targeting glucose-based metabolism. 14. Cancer Metab; 9.
  • Ghazanfari, D., Noori, M., Bergmeier, S., Hines, J., McCall, K., Goetz, D. (2021). A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.. Bioorganic & medicinal chemistry; 40: 116179.
  • Armstrong, I., Aldhumani, A., Schopis, J., Fang, F., Parsons, E., Zeng, C., Hossain, M., Bergmeier, S., Hines, J. (2020). RNA drug discovery: Conformational restriction enhances specific modulation of the T-box riboswitch function. 20. Bioorganic and Medicinal Chemistry; 28: 7. https://api.elsevier.com/content/abstract/scopus_id/85090049585.
  • Roberts, D., Wang, L., Zhang, W., Liu, Y., Shriwas, P., Qian, Y., Chen, X., Bergmeier, S. (2020). Isosteres of ester derived glucose uptake inhibitors. 18. Bioorganic & Medicinal Chemistry Letters; 30: 127406. https://doi.org/10.1016/j.bmcl.2020.127406.
  • Noori, M., Courreges, M., Bergmeier, S., McCall, K., Goetz, D. (2020). Modulation of LPS-induced inflammatory cytokine production by a novel glycogen synthase kinase-3 inhibitor. European Journal of Pharmacology; 883: 173340. https://doi.org/10.1016/j.ejphar.2020.173340.
  • Noori, M., Courreges, M., Bergmeier, S., McCall, K., Goetz, D. (2020). Modulation of LPS-induced inflammatory cytokine production by a novel glycogen synthase kinase-3 inhibitor.. European Journal of Pharmacology; 883: 173340.
  • Roberts, D., Wang, L., Zhang, W., Liu, Y., Shriwas, P., Qian, Y., Chen, X., Bergmeier, S. (2020). Isosteres of ester derived glucose uptake inhibitors.. 18. Bioorganic & medicinal chemistry letters; 30: 127406.
  • Noori, M., Bhatt, P., Courreges, M., Ghazanfari, D., Cuckler, C., Orac, C., McMills, M., Schwartz, F., Deosarkar, S., Bergmeier, S., McCall, K., Goetz, D. (2019). Identification of a novel selective and potent inhibitor of glycogen synthase kinase-3. Am J Physiol - Cell Physiol; 317: C1289-C1303.
  • Bergmeier, S., Zheng, Z. (2019). Routes to N-glycinamide oxazolidinone derivatives: The reaction of 4-trityloxymethyl-3- oxa-1-azabicyclo[3.1.0]hexan-2-one with active halides.. 3. Arkivoc; 1-13.
  • Bergmeier, S., Armstrong, I. (2017). Development of a Method for the Synthesis of 4-Aryl-Functionalized 2-Azabicyclo[3.2.1]octanes. 12. Synthesis; 49: 2733-2742. https://dx.doi.org/10.1055/s-0036-1558973.
  • Noori, M., O'Brien, J., Champa, Z., Deosarkar, S., Lanier, O., Qi, C., Burdick, M., Schwartz, F., Bergmeier, S., McCall, K., Goetz, D. (2017). Phenylmethimazole and a Thiazole Derivative of Phenylmethimazole Inhibit IL-6 Expression by Triple Negative Breast Cancer Cells. European Journal of Pharmacology; 803: 130-137. https://www.sciencedirect.com/science/article/pii/S0014299917302182?via%3Dihub.
  • Fang, F., Maciagiewicz, I., Bergmeier, S. (2016). A synthesis of hexahydro H-oxazolo[3,4-a]pyrazin-3-ones from fused aziridines. 1. Heterocycles; 93.
  • Zeng, C., Zhou, S., Bergmeier, S., Hines, J. (2015). Factors that influence T box riboswitch efficacy and tRNA affinity. Bioorganic & Medicinal Chemistry; 23: 5702-5708.
  • Alapati, A., Deosarkar, S., Lanier, O., Qi, C., Carlson, G., Burdick, M., Schwartz, F., McCall, K., Bergmeier, S., Goetz, D. (2015). Simple Modifications to Methimazole that Enhance its Inhibitory Effect on Tumor Necrosis Factor-alpha-Induced Vascular Cell Adhesion Molecule-1 Expression by Human Endothelial Cells. European Journal of Pharmacology; 751: 59-66.
  • Alapati, A., Deosarkar, S., Lanier, O., Qi, C., Carlson, G., Burdick, M., Schwartz, F., McCall, K., Bergmeier, S., Goetz, D. (2015). Simple modifications to methimazole that enhance its inhibitory effect on tumor necrosis factor-α-induced vascular cell adhesion molecule-1 expression by human endothelial cells.. European journal of pharmacology; 751: 59-66.
  • Malki, A., Laha, R., Bergmeier, S. (2014). Synthesis and cytotoxic activity of MOM-ether analogs of isosteviol. 4. Bioorganic & Medicinal Chemistry Letters; 24: 1184-1187. https://doi.org/10.1016/j.bmcl.2013.12.103.
  • Zhou, S., Means, J., Acquaah-Harrison, G., Bergmeier, S., Hines, J. (2012). 1. Characterization of a 1,4-disubstituted 1,2,3-triazole binding to T box antiterminator RNA . Bioorganic and Medicinal Chemistry; 20: 1298-1302.
  • Fang, F., Roberts, D., Zhou, S., Hines, J., Bergmeier, S. (2012). 2. A synthesis of 1,4-disubstituted Imidazolidin-2-ones from fused-ring aziridines I.W. Maciagiewicz. Synthesis; 44: 551-560.
  • Fang, F., Vogel, M., Hines, J., Bergmeier, S. (2012). 3. Fused ring aziridines as a facile entry into triazole fused tricyclic and bicyclic heterocycles . Org. Biomol. Chemistry; 10: 3080-3091.
  • Liu, Y., Cao, Y., Zhang, W., Bergmeier, S., Qin, Y., Akbar, H., Colvin, R., Ding, J., Tong, L., Wu, S., Hines, J., Chen, X. (2012). 4. A small molecule inhibitor of glucose transporter 1 (Glut1) down-regulates glycolysis, induces cell cycle arrest, and inhibits cancer cell growth in vitro and in vivo . Mol. Cancer Ther; 11: 1672-1682.
  • Bergmeier, S., Wells, G., Huang, J., Katz, S. (2012). Studies on the ring opening reactions of 3-oxa-1-azabicyclo[3.1.0]hexan-2-ones. Synthesis of aminomethyl oxazolidinones and aziridinyl ureas. Tetrahedron; 68: 3980-39887.
  • Bergmeier, S. (2012). 3D-QSAR and 3D-QSSR models of negative allosteric modulators facilitate the design of a novel selective antagonist of human α4β2 neuronal nicotinic acetylcholine receptors. Bioorganic and Medicinal Chemistry Letters; 22: 1797-1813.
  • Bergmeier, S., Huang, J. (2012). An improved synthesis of functionalized cis-dicahydroquinolines using a Baylis- Hillman-type adduct. Heterocycles; 84: 1289-1299.
  • Hurst, W., Krake, S., Bergmeier, S., Payne, M., Miller, K., Stuart, D. (2011). Impact of fermentation, drying, roasting and Dutch processing on flavan-3-ol stereochemistry in cacao beans and cocoa ingredients. 1. Chemistry Central Journal; 5: https://doi.org/10.1186/1752-153x-5-53.
  • Bergmeier, S., McMills, M. (2011). Synthesis of a functionalized oxabicyclo[2.2.1]-heptene-based chemical library. . Combinatorial Chemistry and High-Througput Synthesis; 15: 81-89.
  • Sumskaya, Y., Swain, P., Bergmeier, S., McMills, M., Priestley, N., Wright, D. (2011). Natural feedstocks for diversity-oriented synthesis: macrolide-like scaffolds from nonactate. Arkivoc; 144-166. ://WOS:000290685400013">https://://WOS:000290685400013.
  • Zhou, S., Acquaah-Harrison, G., Bergmeier, S., Hines, J. (2011). Anisotropy studies of tRNA-T box antiterminator RNA complex in the presence of 1,4-disubstituted 1,2,3-triazoles. . Bioorganic and Medicinal Chemistry; 21: 7059-7063.
  • Orac, C., Zhou, S., Means, J., Boehm, D., Bergmeier, S., Hines, J. (2011). Synthesis and stereospecificity of 4,5-disubstituted oxazolidinone ligands binding to T-box riboswitch RNA. 6786-6795. Journal of Medicinal Chemistry; 54.
  • Henderson, B., Orac, C., Maciagiewicz, I., Bergmeier, S., McKay, D. (2011). 3D-QSAR and 3D-QSSR models of negative allosteric modulators facilitate the design of a novel selective antagonist of human α4β2 neuronal nicotinic acetylcholine receptors. . Bioorganic and Medicinal Chemistry Letters; 21: 1797-1813.
  • Maciagiewicz, I., Zhou, S., Bergmeier, S., Hines, J. (2011). Structure activity studies of RNA-binding oxazolidinone derivatives. . Bioorganic and Medicinal Chemistry Letters; 21: 4524-4527.
  • Phillips, J., Smith, A., Kusche, B., Bessette, B., Swain, P., Bergmeier, S., McMills, M., Wright, D., Priestley, N. (2010). Natural product derivatives with bactericidal activity against Gram-positive pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecalis. 19. Bioorganic & Medicinal Chemistry Letters; 20: 5936-5938. ://WOS:000281735600073">https://://WOS:000281735600073.
  • Bergmeier, S., Liu, Y., Cao, Y., Zhang, W., Chen, X. (2010). Small compound inhibitors of basal glucose transport inhibit cell proliferation and induce apoptosis in cancer cells via glucose-deprivation-like mechanisms. . Cancer Lett.; 298: 176-185.
  • Krake, S., Bergmeier, S. (2010). Inter- and intramolecular reactions of epoxides and aziridines with π-nucleophiles. 37. Tetrahedron; 66: 7337-7360. https://doi.org/10.1016/j.tet.2010.06.064.
  • Bergmeier, S., Hines, J., Zhou, S., Acquaah-Harrison, G. (2010). A library of 1,4-disubstituted 1,2,3-triazole analogs of oxazolidinone RNA-binding agents. . 4. J. Comb. Chem.; 12: 491-496.
  • Bergmeier, S., Orac, C. (2010). Negative Allosteric Modulators that Target Human α4β2 Neuronal Nicotinic Receptors. . J. Pharmaco. Exp. Ther.; 334: 761-774.
  • Bergmeier, S., Zhang, W., Chen, X., Liu, Y. (2010). Novel inhibitors of basal glucose transport as potential anticancer agents. Bioorg Med Chem Lett.; 20: 2191-2194.
  • Luesse, S., Wells, G., Nayek, A., Smith, A., Kusche, B., Bergmeier, S., McMills, M., Priestley, N., Wright, D. (2008). Natural products in parallel synthesis: Triazole libraries of nonactic acid. 14. Bioorganic & Medicinal Chemistry Letters; 18: 3946-3949. ://WOS:000257640400025">https://://WOS:000257640400025.
  • Nikodinovic, J., Dinges, J., Bergmeier, S., McMills, M., Wright, D., Priestley, N. (2006). Resolution of methyl nonactate by Rhodococcus erythropolis under aerobic and anaerobic conditions. 3. Organic Letters; 8: 443-445. ://WOS:000235120700023">https://://WOS:000235120700023.
  • Bergmeier, S., Katz, S. (2002). A Method for the Parallel Synthesis of Multiply Substituted Oxazolidinones. 2. Journal of Combinatorial Chemistry; 4: 162-166. https://doi.org/10.1021/cc010050f.
  • Bergmeier, S. (2000). The Synthesis of Vicinal Amino Alcohols. 17. Tetrahedron; 56: 2561-2576. https://doi.org/10.1016/s0040-4020(00)00149-6.
  • Bergmeier, S., Fundy, S. (1997). Synthesis of oligo(5-aminopentanoic acid)-nucleobases (APN): potential antisense agents. 24. Bioorganic & Medicinal Chemistry Letters; 7: 3135-3138. https://doi.org/10.1016/s0960-894x(97)10172-x.
  • Moos, W., Bergmeier, S., Coughenour, L., Davis, R., Hershenson, F., Kester, J., McKee, J., Marriott, J., Schwarz, R., Tecle, H., Thomas, A. (1992). Cholinergic Agents: Effect of Methyl Substitution in a Series of Arecoline Derivatives on Binding to Muscarinic Acetylcholine Receptors. 10. Journal of Pharmaceutical Sciences; 81: 1015-1019. https://doi.org/10.1002/jps.2600811012.

Journal Article, Professional Journal (1)

  • McMills, M., Bergmeier, S. (2010). Natural Prtoduct Derivatives with Bactericidal Activity Against Gram-positive Pathogens Including Methicillin-resistant Staphylococcus aureus and Vancomycin-resistant Enterococcus faecalis. 19. Bioorganic and Medicinal Chemistry Letters/Elsevier; 20: 5936-5938.

Patent Publications (10)

  • Goetz, D., Begmeier, S., McMills, M., Orac, C. Imidazole and thiazole compositions for modifying biological signaling . 10,633,377.
  • Goetz, D., Bergmeier, S., McMills, M., Orac, C. Imidazole and thiazole compositions for modifying biological signaling -B. 10,407,420.
  • Goetz, D., Bergmeier, S., McMills, M., Orac, C. Imidazole and thiazole compositions for modifying biological signaling - C . Application # 20200017489.
  • McMills, M., Goetz, D., Bergmeier, S., Orac, C. Imidazole and Thiazole Compositions for Modifying Biological Signaling . 10,023,567.
  • Bergmeier, S., Chen, X. Compositions and methods for glucose transport inhibition. US 10,000,443, B2.
  • Bergmeier, S., Chen, X. Compositions and Methods for Glucose Transport Inhibition. US Patent 9181162.
  • Goetz, D., McCall, K., Bergmeier, S., Schwartz, F., Bhatt, P., Deosarkar, S. Methods and compositions to modify GSK-3 activity.
  • Bergmeier, S., Goetz, D., McMall, K. A method to modify the activity of GSK-3.
  • Bergmeier, S., Goetz, D., McMall, K. Use of phenylmethyimazole for the prevention and treatment of fatty liver disease.
  • Bergmeier, S., Goetz, D., McMills, M., McMall, K. Compositions that modify biological signaling.

Book, Chapter in Scholarly Book (3)

  • Bergmeier, S. (2013). Three-membered ring systems. Elsevier; 25: 47-70.
  • Bergmeier, S. (2011). Three-membered ring systems. Progress in Heterocyclic Chemistry; 23: 75-100.
  • Bergmeier, S., Lapinsky, D. (2010). Three-membered ring systems. . Progress in Heterocyclic Chemistry; 22: 59-83.