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Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors.

Yin, Zheng and Patel, Sejal and Wang, Wei and Chan, Wai Ling and Rao, Ranga and Wang, Gang and Ngew, Xinyi and Patel, Viral and Beer, David and Knox, John E and Ma, Ngai Ling and Ehrhardt, Claus and Lim, Siew Pheng and Vasudevan, Subhash and Keller, Thomas (2006) Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors. Bioorganic & Medicinal Chemistry Letters, 16 (1). pp. 40-43. ISSN 0960-894X

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.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Dengue virus NS3 protease; Peptide inhibitors
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Date Deposited: 14 Dec 2009 14:01
Last Modified: 31 Jan 2013 01:20
URI: https://oak.novartis.com/id/eprint/315

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