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An expedient synthesis of N α -protected- l -tetrahydrofuranylglycine and its application in the synthesis of novel substrate based inhibitors of HIV-1 protease

Bioorganic & Medicinal Chemistry Letters, ISSN: 0960-894X, Vol: 12, Issue: 24, Page: 3615-3617
2002
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Z- and Fmoc- l -tetrahydrofuranylglycines have been obtained from l -vinylglycine through dipolar cycloaddition reaction, and its Fmoc derivative has been applied in the synthesis of modified S9 and S10 substrates of HIV-1 protease. These compounds mostly acted as strong inhibitors, rather than substrates, of the protease, probably due to the favourable interactions of the tetrahydrofuranylglycine moiety at the S 2 site.

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