| Literature DB >> 16246563 |
Zheng Yin1, Sejal J Patel, Wei-Ling Wang, Wai-Ling Chan, K R Ranga Rao, Gang Wang, Xinyi Ngew, Viral Patel, David Beer, John E Knox, Ngai Ling Ma, Claus Ehrhardt, Siew Pheng Lim, Subhash G Vasudevan, Thomas H Keller.
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.Entities:
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Year: 2005 PMID： 16246563 DOI： 10.1016/j.bmcl.2005.09.049
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823