2. Academic Validation
  3. Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors

Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors

  • ACS Med Chem Lett. 2015 Jan 25;6(3):359-62. doi: 10.1021/acsmedchemlett.5b00008.
Song Feng 1,  Di Hong 1,  Baoxia Wang 1,  Xiufang Zheng 1,  Kun Miao 1,  Lisha Wang 1,  Hongying Yun 1,  Lu Gao 1,  Shuhai Zhao 1,  Hong C Shen 1
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Molecular Design and Chemical Biology, and Infectious Diseases, Pharmaceutical Research and Early Development, Roche Innovation Center Shanghai , Building 5, Lane 720, Cai Lun Road, Shanghai 201203, China.
PMID: 25941547 DOI: 10.1021/acsmedchemlett.5b00008
Abstract

A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and physical-chemical properties. Several highly potent compounds such as 8ji, 8jl, and 8jm were identified with single nanomolar activities. The most potent compound 8jm showed an IC50 of 3 nM, lower microsome clearance and no CYP inhibition. The profile of 8jm appeared to be superior to BMS433771, and supported further optimization.

Keywords

Respiratory syncytial virus (RSV); antiviral; fusion inhibitors; heterocycle; imidazopyridine; virus.

Figures