tetano
Editor, Senior Moderator
ChemMedChem. 2012 Jul 23. doi: 10.1002/cmdc.201200259. [Epub ahead of print]
Anti-influenza Drug Discovery: Identification of an Orally Bioavailable Quinoline Derivative through Activity- and Property-Guided Lead Optimization.
Yeh JY, Coumar MS, Shiao HY, Lin TJ, Lee YC, Hung HC, Ko S, Kuo FM, Fang MY, Huang YL, Hsu JT, Yeh TK, Shih SR, Chao YS, Horng JT, Hsieh HP.
Source
Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Rd, Zhunan, Miaoli County 350 (Taiwan, RoC).
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.
Copyright ? 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
PMID:
22821876
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/22821876
Anti-influenza Drug Discovery: Identification of an Orally Bioavailable Quinoline Derivative through Activity- and Property-Guided Lead Optimization.
Yeh JY, Coumar MS, Shiao HY, Lin TJ, Lee YC, Hung HC, Ko S, Kuo FM, Fang MY, Huang YL, Hsu JT, Yeh TK, Shih SR, Chao YS, Horng JT, Hsieh HP.
Source
Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Rd, Zhunan, Miaoli County 350 (Taiwan, RoC).
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.
Copyright ? 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
PMID:
22821876
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/22821876