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Medicinal and Biological Chemistry
Paul W. Erhardt
|B.A., Chemistry, 1969||University of Minnesota|
|Ph.D., Medicinal Chemistry, 1974||University of Minnesota|
|Post-doctoral Research Associate, 1974-1975||University of Texas at Austin|
Synthetic medicinal agents; organic and peptidomimetic compounds; small-ring scaffold systems; nitrogen asymmetry and racemic inversion; 'metabophore' technologies.
Our group is interested in three major areas. The first involves translating information about biochemical pathways into practical, small organic or peptidomimetic therapeutic agents. Today's explosion of biotechnology-related information has provided a plethora of such opportunities. As a result, it is possible to select problems which can be esthetically pleasing at the molecular level (e.g., those which may be amenable to approaches involving small, symmetrical scaffolds), as well as having the potential to make a major impact upon the health of man (e.g., choosing problems in a major disease category which has eluded adequate therapeutic intervention). One of our ongoing programs in this area involves pursuit of small-molecule versions of the new anticancer agent paclitaxel (1).
A second area of interest involves constructing appendant molecular systems which rely upon in vivo metabolic processes ('metabophores') to alter the properties of their parent drugs in a programmed manner so as to enhance the overall therapeutic profiles of the new composite molecules. This technology has numerous applications, but is particularly useful when combined with topical and critical care medications, as was done successfully in the design of the ultra-short-acting beta-adrenergic receptor blocking agent esmolol (2).
Finally, a third area of interest involves developing rational libraries of molecular probes which can be utilized to survey receptor topographies and to provide initial lead structures during the early phases of drug discovery.
AsDirector of the CD3 my involvement encompasses all aspects of pharmaceutical research and development, ranging from the design and synthesis of small-molecule therapeutics to the advanced clinical study of marketed drugs and diagnostic agents. In this capacity, the CD3 participates in a wide range of collaborative research activities throughout the University and its immediately surrounding medical research community.
- Erhardt, P. and Y-L. Chou. Topographical model for the cAMP phosphodiesterase III
active site. Life Sciences 49, 553, 1991.
- Shaw, K., P. Erhardt, A. Hagedorn, C. Pease, W. Ingebretsen and J. Wiggins. Cardiotonic
agents 7. Prodrug derivatives of 4-ethyl-1,3-dihydro-5-[4-(2-methyl)-1H-imidazol-1-yl)benzoyl]-2H-imidazole-2-one.
J. Med. Chem. 35, 1267, 1992.
- Erhardt, P. Endothelin structure and structure-activity relationships. In Endothelin, C. Rubanyi, Ed., Oxford University Press, London, 1992.
- Lampe, J., Y.-L. Chou, R. Hanna, S. DiMeo, P. Erhardt, A. Hagedorn III, W. Ingebretsen
and E. Cantor. (Imidazolylphenyl)pyrrol-2-one Inhibitors of Cardiac cAMP Phosphodiesterase.
J. Med. Chem. 36, 1041, 1993.
- Erhardt, P. Esmolol. In Chronicles of Drug Discovery. D. Lednicer, Ed. ACS Books, Washington, D.C., 1993
- Bihovsky, R., B. Levinson, R. Loewi, P. Erhardt and M. Polokoff. Hydroxamic acids
as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth
muscle. J. Med. Chem. 38, 2119-2129, 1995.
- Bihovsky, R., P. Erhardt, J. Lampe, R. Mohan and K. Shaw. Inhibitors of the conversion
of big endothelin to endothelin. U.S. Patent 5 504 070, 1996.
- Erhardt, P. The Biochemical Mechanism of Paclitaxel: In Pursuit of a Microtubule Binding
Site. The Taxane Journal 3: 36-42,1997.
- Erhardt, P. Chemotherapeutic Agents. Lecture 1. Am. J. Pharmaceut. Ed., 61, 192-196,1997.
- Hu, Z. and P. Erhardt. Utilization of a Benzoyl Migration to Effect an Expeditious
Synthesis of the Paclitaxel Side Chain Org. Process Res. & Develop., 387-390,1997.
- Sarver J., R. Pryka, K. Alexander, L. Weinstein and P. Erhardt Stability of Magnesium
Sulfate in 0.9% Sodium Chloride and Lactated Ringers Solutions. Int. J. Pharmaceutical Compd., 2, 385-388,1998.
- Erhardt, P. Drug Metabolism Data: Past and Present Status., Medicinal Chemistry Research 8: 7-8, 400-421,1998.
- Erhardt, P. Benzylamine-Related Chiral Auxiliary Synthetic Reagents.. U.S. Patent,
- J. Sarver, N. Peng, S. Lerdkanchanaporn, K. Oravecz-Wilson, K. Alexander and P. Erhardt.
Analysis of Extemporaneous Alprostadil Formulations Intended for the Treatment of
Erectile Dysfunction Int. J. Pharmaceutical Compd. 3:148-155,1999.
- Drug Metabolism Data: Past, Present and Future Considerations. P. Erhardt. In Drug
Metabolism: Databases and High Throughput Testing During Drug Design and Development,
ed. by P. Erhardt, IUPAC/Blackwell, Geneva, 1999.
- Case Studies: A Prodrug and a Softdrug. P. Erhardt. In Drug Metabolism: Databases
and High Throughput Testing During Drug Design and Development, ed. by P. Erhardt,
- Prodrugs and Codrugs T. Wilbury (P. Erhardt et al.) In Drug Metabolism: Databases
and High Throughput Testing During Drug Design and Development,ed. by P. Erhardt,
IUPAC/Blackwell, Geneva, 1999.
- Statistics-Based Probabilities of Metabolic Possibilities. P. Erhardt. In Drug Metabolism:
Databases and High Throughput Testing During Drug Design and Development, ed. by P.
Erhardt, IUPAC/Blackwell, Geneva, 1999.
- Drug Metabolism: Databases and High Throughput Testing During Drug Design and Development.
Served as organizer and editor for entire text which has over 50 international expert
contributors. Published by IUPAC/Blackwell, Geneva, 1999.
- Z. Hu, M.J. Hardie, P. Burckel, A.A. Pinkerton and P.W. Erhardt Conversion of 2,4-Dihydroxybenzaldehyde
to 2-Benzoyloxy-4-hydroxybenzaldehyde and their Structural Characterization. J. Chem.
Crystallog., 29, 185-191, 1999.
- Methods For Producing Two-Substituted Glycerols Having Various Levels of Protection.
P. Erhardt and W. Klis. U.S. Patent Application, Filed 2000.
- Aralkyl Ester Softdrugs. P. Erhardt. U.S. Patent Application, Filed 2000.
- AConvenient Synthesis of 2-Phenylglycerol. P. Erhardt and W. Klis. Synth. Comm., Accepted.
- 2-Phenylglycerol: Crystal Structure and Conformational Considerations Pertaining to
Formation of Its Related Oxetane. P.W. Erhardt, W.A. Klis, P.I. Nagy, K. Kirschbaum,
N. Wu, A. Martin and A.A. Pinkerton. J. Chem. Crystallog, accepted.
- Metabolism Prediction. P. Erhardt. Bio Techniques, Accepted. Reproducibility of the High-Performance Liquid Chromatographic Fingerprints Obtained From Two Soybean Cultivars and a Selected Progeny. J. Faghihi, X. Jiang, R. Vierling, S. Goldman, S. Sharfstein and P. Erhardt. J. Chrom. A submitted.