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Discovery of (aza)indole derivatives as novel respiratory syncytial virus fusion inhibitors

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Abstract

A new class of indole derivatives (3) have been identified as potent RSV fusion inhibitors. SAR exploration revealed that 5-Cl and the sulfonyl side chain of the indole scaffold are crucial for anti-RSV activity. Further optimization led to the discovery of a cyclic sulfone (8i) with 2 nM anti-RSV activity and a much improved PK profile compared to the non-cyclic sulfone counterpart.

Graphical abstract: Discovery of (aza)indole derivatives as novel respiratory syncytial virus fusion inhibitors

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Publication details

The article was received on 26 Mar 2019, accepted on 30 Apr 2019 and first published on 06 May 2019


Article type: Research Article
DOI: 10.1039/C9MD00178F
Med. Chem. Commun., 2019, Advance Article

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    Discovery of (aza)indole derivatives as novel respiratory syncytial virus fusion inhibitors

    X. Zheng, C. Liang, L. Wang, K. Miao, B. Wang, W. Zhang, D. Chen, G. Wu, W. Zhu, L. Guo, S. Feng, L. Gao, H. C. Shen and H. Yun, Med. Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9MD00178F

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