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One-port Synthesis Of Hydroxide Peptides And Cyclic Peptides By Volatilizable Silica Gel

Posted on:2008-06-21Degree:MasterType:Thesis
Country:ChinaCandidate:J SunFull Text:PDF
GTID:2144360242475755Subject:Medicinal chemistry
Abstract/Summary:PDF Full Text Request
Cyclic peptides form a particular class of compounds with multiple and varied biological functions. These cyclic peptides act as potent antimicrobial, cytotoxic, antineoplastic, and antiviral agents of great therapeutic value. Cyclic peptides, in particular, attracted our attention as designer targets because of their demonstrated potential as antibiotics, regulators of membrane ion transport, and templates for protein design. During middle of the 20th centuries, some scientists had separated a few kinds of cyclic peptides and completed total synthesis of these cyclic peptides. More cyclic peptides were found during the past 40 years. The conformational constraints of cyclic peptides have allowed them to serve as useful and predictable models of various protein structural motifs, includingβ-foldingβ-turn andγ-turn. They can also provide the elements required to delineate ligand-receptor and enzyme substrate/inhibitor interactions for a multitude of processes.Since it is difficult to get natural cyclic peptides by seperation, we have to use total synthesis in order to attain more cyclopeptides. With the development of new method and efficient coupling reagents, the synthesis of cyclopeptides has great changed. There are several ways to synthesize cyclic peptides; all of them have advantages and disadvantages.We use functional silica gel as volatilizable support and linker and react with several amino acids. Finally we get hydroxide peptides and cyclic peptides. Our method is exemplified by the solid-phase synthesis on "volatilizable" solid supports and linkers that can be completely removed by their ultimate decomposition and complete "volatilization" during the final cleavage step of the synthetic process. This approach eliminates the final extraction step and yields solely the desired synthetic product(s) in the reaction vessel. This method is suitable for the parellel synthesis and automatic synthesis of compound library used for screening.With the development of human genome, proteome and high throughout screening system, cyclic peptides play a vital role in study and mimicry of protein folding. We should try to find a more efficient method, resin and coupling reagent to synthesize cyclic peptides.
Keywords/Search Tags:hydroxide peptides, cyclic peptide, solid-phase synthesis, "volatilizable" solid supports
PDF Full Text Request
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