William Groutas

William C. Groutas

Distinguished Professor
Bioorganic and Medicinal Chemistry
Endowment Association's Distinguished Professor
Ph.D., University of Kentucky, 1973

Tel: 316.978.7374
Fax: 316.978.3431
Email: Bill.Groutas@wichita.edu

Research Interests

  • Structure-based desin and synthesis of inhibitors of neutrophil-derived proteolytic enzymes involved in inflammatory diseases.
  • Application of high-field NMR in the study of enzyme-substrate and enzyme-inhibitor interactions.
  • Use of computational chemistry and computer graphics and modeling in drug design.

Combinatorial Chemistry

An array of inflammatory disease are associated with a massive influx of neutrophils, the release of chemokines, the production of reactive oxygen species, and a compromised proteinase/ antiproteinase screen. The inflammatory process also involves the extracellular release of the lysosomal serine enopeptidases alastase, cathepsin G, and proteinase Poor control of the activity of these enzymes due to depressed levels of their endogenous inhibitors is believed to result in the destruction of the major components of connective tissue. We are interested in the design of mechanism-based inhibitors of these and related serine endopeptidases.

Computer generated molecule diagram. Computer generated molecule diagram. Computer generated molecule diagram. Diagram of a molecule.

Selected Publications

  • R. Kuang, J. B. Epp, S. Ruan, L.S. Chong, R. Venkataraman, J. Tu, S. He, T. M. Truong, W. C. Groutas (2000) Utilization of the 1,2,5-Thiadiazolidin-3-one 1,1 Dioxide Scaffold in the Design Potent Inhibitors of Serine Proteases: SAR Studies Using Carboxylates Bioorg. Med. Chem., in press.
  • W. C. Groutas Organic Reaction Mechanisms, John Wiley & Sons (2000).
  • W. C. Groutas, N. M. Schechter, S. He, H. Yu, P. Huang, J. Tu (1999) Human Chymase Inhibitors Based on the 1,2,5-Thiadiazolidin-3-one 1,1 Dioxide Scaffold Bioorg. Med. Chem. Lett. 9, 2199-2204.
  • R. Kuang, J. B. Epp, S. Ruan, H. Yu, P. Huang, S. He, J. Tu, N. M. Schechter, J. Turbov, C. J. Froelich, W. C. Groutas (1999) A Universal Scaffold for Serine Proteinases with a (Chymo)trypsin-like Fold: Solution Phase Construction and