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Discovery of 2-oxopiperazine dengue inhibitors by scaffold morphing of a phenotypic high-throughput screening hit

Kounde, Cyrille Stephane and Yeo, Hui Quan and Wang, Qingyin and Wan, Kah Fei and Dong, Hongping and Karuna, Ratnaningrum and Dix, Ina and Wagner, Beatrix and Zou, Bin and Simon, Oliver and Bonamy, Ghislain M. C. and Yeung, Bryan King Sing and Yokokawa, Fumiaki (2017) Discovery of 2-oxopiperazine dengue inhibitors by scaffold morphing of a phenotypic high-throughput screening hit. Bioorganic and Medicinal Chemistry Letters, 27 (6). pp. 1385-1389. ISSN 1464-3405

Abstract

A series of 2-oxopiperazine derivatives were designed from the pyrrolopiperazinone cell-based screening hit 4 as a dengue virus inhibitor. Systematic investigation of the structure-activity relationship (SAR) around the piperazinone ring led to the identification of compound (S)-29, which exhibited potent anti-dengue activity in the cell-based assay across all four dengue serotypes with EC50 < 0.1 μM. Cross-resistant analysis confirmed that the virus NS4B protein remained the target of the new oxopiperazine analogs obtained via scaffold morphing from the HTS hit 4.

Item Type: Article
Keywords: 2-Oxopiperazine Cell-based screen Dengue virus NS4B Scaffold morphing
Date Deposited: 14 Mar 2018 00:45
Last Modified: 25 Jan 2019 00:45
URI: https://oak.novartis.com/id/eprint/31802

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