Discovery of (aza)indole derivatives as novel respiratory syncytial virus fusion inhibitors,10.1039/C9MD00178F

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Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

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

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

MedChemComm Pub Date : 05/06/2019 00:00:00 , DOI:10.1039/C9MD00178F

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.