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

ID: ALA4373654

Journal: Medchemcomm

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

Authors: Zheng X, Liang C, Wang L, Miao K, Wang B, Zhang W, Chen D, Wu G, Zhu W, Guo L, Feng S, Gao L, Shen HC, Yun H.

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.

CiteXplore: 31303995

DOI: 10.1039/C9MD00178F

Patent ID: ┄