期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 16, 页码 4538-4541出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.009
关键词
SARS (Severe Acute Respiratory Syndrome); NTPase/helicase; Dihydroxychromone; Pharmacophore
资金
- Ministry for Health, Welfare & Family Affairs, Republic of Korea [A08-4628-AA2023-08N1-00010A]
- ORP [11-30-68]
- Korea Ministry of Agriculture and Forestry
- Korean Government [KRF-2008-313-C00531]
- Kookmin University in Korea
Aryl diketoacids have been identified as the first SARS-CoV NTPase/helicase inhibitors with a distinct pharmacophore featuring an arylmethyl group attached to a diketoacid. In order to search for the pharmacophore space around the diketoacid core, three classes of dihydroxychromone derivatives were prepared. Based on SAR study, an extended feature of the pharmacophore model of SARS-CoV NTPase/helicase was proposed which is constituted of a diketoacid core, a hydrophobic arylmethyl substituent, and a free catechol unit. (C) 2009 Elsevier Ltd. All rights reserved.
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