Investigation of the pharmacophore space of Severe Acute Respiratory Syndrome coronavirus (SARS-CoV) NTPase/helicase by dihydroxychromone derivatives

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...

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Detalles Bibliográficos
Autores principales: Lee, Chaewoon, Lee, Jin Moo, Lee, Na-Ra, Kim, Dong-Eun, Jeong, Yong-Joo, Chong, Youhoon
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2009
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7127646/
https://www.ncbi.nlm.nih.gov/pubmed/19625187
http://dx.doi.org/10.1016/j.bmcl.2009.07.009
Descripción
Sumario: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.

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