1.
ACS Med Chem Lett
; 9(4): 397, 2018 04 12.
Article
in English
| MEDLINE
| ID: mdl-29671838
ABSTRACT
[This corrects the article DOI: 10.1021/acsmedchemlett.7b00418.].
2.
ACS Med Chem Lett
; 9(2): 94-97, 2018 Feb 08.
Article
in English
| MEDLINE
| ID: mdl-29456794
ABSTRACT
A new series of 3,3'-spirocyclic-2-oxo-indoline derivatives was synthesized and evaluated against respiratory syncytial virus (RSV) in a cell-based assay and animal model. Extensive structure-activity relationship study led to a lead compound 14h, which exhibited excellent in vitro potency with an EC50 value of 0.8 nM and demonstrated 71% oral bioavailability in mice. In a mouse challenge model of RVS infection, 14h demonstrated superior efficacy with a 3.9log RSV virus load reduction in the lung following an oral dose of 50 mg/kg.