Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors.
Basic Information
ID: ALA1147782
Journal: Bioorg Med Chem Lett
Title: Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors.
Authors: Yin Z, Patel SJ, Wang WL, Chan WL, Ranga Rao KR, Wang G, Ngew X, Patel V, Beer D, Knox JE, Ma NL, Ehrhardt C, Lim SP, Vasudevan SG, Keller TH.
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, K(i)=5.8 microM). In general, we observe that interactions of P(2) side chain are more important than P(1) followed by P(3) and P(4). Tripeptide and dipeptide aldehyde inhibitors also show low micromolar activity. Additionally, an effective non-basic, uncharged replacement of P(1) Arg is identified.
CiteXplore: 16246563
DOI: 10.1016/j.bmcl.2005.09.049
Patent ID: ┄