ORGN 310 |
| Small biologically active peptides are often highly flexible molecules that undergo rapid conformational inter-conversions. The introduction of conformational constraints into these peptides, so that particular backbone conformations are enforced, is one of most promising avenues for probing peptide-receptor interaction. As part of our ongoing efforts to develop protocols for the parallel synthesis of bioactive small molecules for drug discovery, we have recently developed a synthetic strategy using sequential Ugi/RCM/1,3-dipolar cycloaddition reactions to construct conformationally constrained peptide motifs. A series of bicyclic lactam tri-peptide libraries have been synthesized in the spirit of diversity-oriented synthesis. The experimental results and discussion will be presented.
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Combinatorial, Parallel, and Solid-Phase Chemistry
1:00 PM-5:20 PM, Tuesday, 28 March 2006 Georgia World Congress Center -- C302, Oral
Division of Organic Chemistry |
