Efficient synthesis and anti-enteroviral activity of 9-arylpurines

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.status: publishe

Efficient synthesis and anti-enteroviral activity of 9-arylpurines

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 EC50 values varying from 3 to 15 mM, 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.L.A. thanks the Spanish Ministerio de Educación y Ciencia (MEC) for an FPU predoctoral fellowship. M.-C. C. thanks the Fondo Social Europeo (FSE) and the JAE Predoc Programme for a predoctoral fellowship. We thank Ms. María Nares for excellent technical assistance and the support of the Spanish MEC and the Fondo Social Europeo (FSE). This project has been supported by the Spanish CICYT (SAF2009-13914-C02-01). We also would like to acknowledge Stijn Delmotte, Tom Bellon, Mieke Flament, and Annelies De Ceulaer for their excellent technical assistance in the acquisition of the antiviral data.Peer reviewe