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

MedChemComm, ISSN: 2040-2511, Vol: 10, Issue: 6, Page: 970-973
2019
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Article Description

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.

Bibliographic Details

Zheng, Xiufang; Liang, Chungen; Wang, Lisha; Miao, Kun; Wang, Baoxia; Zhang, Weixing; Chen, Dongdong; Wu, Guolong; Zhu, Wei; Guo, Lei; Feng, Song; Gao, Lu; Shen, Hong C; Yun, Hongying

Royal Society of Chemistry (RSC)

Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics; Chemistry

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