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
  • 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.

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