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

Autor:	Hsing Pang Hsieh, Fu Ming Kuo, Ming Yu Fang, Teng Kuang Yeh, Jim-Tong Horng, Ta Jen Lin, Shengkai Ko, Mohane Selvaraj Coumar, Shin-Ru Shih, Hui Chen Hung, Yu-Sheng Chao, Yen Chun Lee, Yu Lin Huang, Hui Yi Shiao, John T.A. Hsu, Jiann Yih Yeh
Rok vydání:	2012
Předmět:	Male Pharmacology Biochemistry Antiviral Agents Cell Line Rats Sprague-Dawley chemistry.chemical_compound Structure-Activity Relationship Influenza A Virus H1N1 Subtype Pharmacokinetics Orthomyxoviridae Infections Drug Discovery Influenza Human Animals Humans General Pharmacology Toxicology and Pharmaceutics Drug discovery Organic Chemistry Quinoline Lead Agent Bioavailability Rats chemistry Anti influenza drug Quinolines Molecular Medicine Derivative (chemistry)
Zdroj:	ChemMedChem. 7(9)
ISSN:	1860-7187
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acede49520cce70e3e8b876f62807686 https://pubmed.ncbi.nlm.nih.gov/22821876 Zobrazit plný text záznamu Plný text