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Anti‐influenza Drug Discovery: Identification of an Orally Bioavailable Quinoline Derivative through Activity‐ and Property‐Guided Lead Optimization
Author(s) -
Yeh JiannYih,
Coumar Mohane Selvaraj,
Shiao HuiYi,
Lin TaJen,
Lee YenChun,
Hung HuiChen,
Ko Shengkai,
Kuo FuMing,
Fang MingYu,
Huang YuLin,
Hsu John T. A.,
Yeh TengKuang,
Shih ShinRu,
Chao YuSheng,
Horng JimTong,
Hsieh HsingPang
Publication year - 2012
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201200259
Subject(s) - lead compound , bioavailability , drug , drug discovery , lead (geology) , pharmacology , chemistry , medicine , biochemistry , biology , in vitro , paleontology
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.