1. Academic Validation
  2. Efficient synthesis and anti-enteroviral activity of 9-arylpurines

Efficient synthesis and anti-enteroviral activity of 9-arylpurines

  • Eur J Med Chem. 2012 Mar:49:279-88. doi: 10.1016/j.ejmech.2012.01.022.
Leire Aguado 1 María-Dolores Canela Hendrik Jan Thibaut Eva-María Priego María-José Camarasa Pieter Leyssen Johan Neyts María-Jesús Pérez-Pérez
Affiliations

Affiliation

  • 1 Instituto de Química Médica (IQM-CSIC), Madrid, Spain.
Abstract

To further explore the anti-enteroviral activity of 9-aryl-6-chloropurines, three different series of compounds with a dialkylamino, (alkyl)amido, or Oxazolidinone substituent at the aryl ring have been synthesized, in most cases with the aid of microwave-assisted synthesis. The resulting compounds efficiently inhibit Coxsackie virus type B3 (CVB3) replication with EC(50) values varying from 3 to 15 μM, and with no significant toxicity in Vero cells. The most potent compounds also selectively inhibit the replication of Other enteroviruses including Coxsackie virus B4 and Echo virus 11. The cross-resistance studies performed with different 9-aryl-6-chloropurines indicate that they all belong to the same pharmacological family and differ from Other CVB3 drugs such as enviroxime.

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