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Endothiopeptide inhibitors of HIV-1 protease
S Yao1, R Zutshi, J Chmielewski
1Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
Endothiopeptide inhibitors of HIV-1 protease were synthesized by chemical and enzymatic methods to individually replace each backbone amide bond in 1 with a thioamide-linkage. Interestingly, agent 7, which contains a thioamide-linkage between the P2' and P3' positions of 1, was the most potent, competitive inhibitor of HIV-1 protease with a Ki of 3.4 microM.