Title of article
Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors
Author/Authors
Zheng Yin، نويسنده , , Sejal J. Patel، نويسنده , , Wei-Ling Wang، نويسنده , , Wai-Ling Chan، نويسنده , , K.R. Ranga Rao، نويسنده , , Gang Wang، نويسنده , , Xinyi Ngew، نويسنده , , Viral Patel، نويسنده , , David Beer، نويسنده , , John E. Knox، نويسنده , , Ngai Ling Ma، نويسنده , , Claus Ehrhardt، نويسنده , , Siew Pheng Lim، نويسنده , , Subhash G. Vasudevan and David L. Ollis، نويسنده , , Thomas H. Keller، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
40
To page
43
Abstract
With the aim of discovering potent and selective dengue NS3 protease inhibitors, we systematically synthesized and evaluated a series of tetrapeptide aldehydes based on lead aldehyde 1 (Bz-Nle-Lys-Arg-Arg-H, Ki = 5.8 μM). In general, we observe that interactions of P2 side chain are more important than P1 followed by P3 and P4. Tripeptide and dipeptide aldehyde inhibitors also show low micromolar activity. Additionally, an effective non-basic, uncharged replacement of P1 Arg is identified.
Keywords
Dengue virus NS3 protease , Peptide inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796308
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