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

Medchemcomm. 2019;

ZhengXiufang，LiangChungen，WangLisha，MiaoKun，WangBaoxia，ZhangWeixing，ChenDongdong，WuGuolong，ZhuWei，GuoLei，FengSong，GaoLu，ShenHong C，YunHong

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Custom Vector Construction	… image file: c9md00178f-f2.tif. Fig. 2 8i inhibited RSV F protein-induced fusion process. The F gene of RSV Long strain was codon-optimized and synthesized by GenScript. The full length of the F gene was cloned into the pcDNA5 TOPO TA vector (Invitrogen) …	Get A Quote

摘要

A new class of indole derivatives () 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 () with 2 nM anti-RSV activity and a much improved PK profile compared to the non-cyclic sulfone counterpart.