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
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.
University of Illinois - Urbana-Champaign
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University of Illinois at Urbana-Champaign