I.~Design, Synthesis, and Evaluation of a Rigidly Constrained Peptidomimetic as a Potential Type I Beta-Turn. II.~Development of Novel Estrogen Receptor Ligands With Unique Endocrine Profiles. III.~Design, Synthesis and Biological Evaluation of Potential Aspartic Protease Inhibitors Based on the Diaziridine and Diazirine Isostere

Fink, Brian Edward

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Description

Title

I.~Design, Synthesis, and Evaluation of a Rigidly Constrained Peptidomimetic as a Potential Type I Beta-Turn. II.~Development of Novel Estrogen Receptor Ligands With Unique Endocrine Profiles. III.~Design, Synthesis and Biological Evaluation of Potential Aspartic Protease Inhibitors Based on the Diaziridine and Diazirine Isostere

Author(s)

Fink, Brian Edward

Issue Date

1998

Doctoral Committee Chair(s)

Katzenellenbogen, John A.

Department of Study

Chemistry

Discipline

Chemistry

Degree Granting Institution

University of Illinois at Urbana-Champaign

Degree Name

Ph.D.

Degree Level

Dissertation

Keyword(s)

Biology, Animal Physiology

Language

eng

Abstract

We have prepared novel aspartic proteases inhibitors based on the diaziridine and diazirine isostere, as potential transition-state mimics of the tetrahedral intermediate found along the reaction pathway for enzyme mediated peptide bond hydrolysis. These isosteres (143 and 144) have been incorporated into substrates for the aspartic protease pepsin, however they did not show any inhibition.

Graduation Semester

1998

Type of Resource

text

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