2. Academic Validation
  3. Anti-influenza drug discovery: identification of an orally bioavailable quinoline derivative through activity- and property-guided lead optimization

Anti-influenza drug discovery: identification of an orally bioavailable quinoline derivative through activity- and property-guided lead optimization

  • ChemMedChem. 2012 Sep;7(9):1546-50. doi: 10.1002/cmdc.201200259.
Jiann-Yih Yeh 1,  Mohane Selvaraj Coumar,  Hui-Yi Shiao,  Ta-Jen Lin,  Yen-Chun Lee,  Hui-Chen Hung,  Shengkai Ko,  Fu-Ming Kuo,  Ming-Yu Fang,  Yu-Lin Huang,  John T A Hsu,  Teng-Kuang Yeh,  Shin-Ru Shih,  Yu-Sheng Chao,  Jim-Tong Horng,  Hsing-Pang Hsieh
Affiliations

Affiliation

  • 1 Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Rd, Zhunan, Miaoli County 350, Taiwan, RoC.
PMID: 22821876 DOI: 10.1002/cmdc.201200259
Abstract

From a high-throughput screening (HTS) hit with inhibitory activity against virus-induced cytophathic in the low micromolar range, we have developed a potent anti-influenza lead through careful optimization without compromising the drug-like properties of the compound. An orally bioavailable compound was identified as a lead agent with nanomolar activity against influenza, representing a 140-fold improvement over the initial hit.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-161356
    RNA-dependent RNA Polymerase Inhibitor