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Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents

Tardugno, Roberta, Giancotti, Gilda, De Burghgraeve, Tine, Delang, Leen, Neyts, Johan, Leyssen, Pieter, Brancale, Andrea and Bassetto, Marcella 2018. Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents. Bioorganic and Medicinal Chemistry 26 (4) , pp. 869-874. 10.1016/j.bmc.2018.01.002

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Chikungunya virus is a re-emerging arbovirus transmitted to humans by mosquitoes, responsible for an acute flu-like illness associated with debilitating arthralgia, which can persist for several months or become chronic. In recent years, this viral infection has spread worldwide with a previously unknown virulence. To date, no specific antivirals treatments nor vaccines are available against this important pathogen. Starting from the structures of two antiviral hits previously identified in our research group with in silico techniques, this work describes the design and preparation of 31 novel structural analogues, with which different pharmacophoric features of the two hits have been explored and correlated with the inhibition of Chikungunya virus replication in cells. Structure-activity relationships were elucidated for the original scaffolds, and different novel antiviral compounds with EC50 values in the low micromolar range were identified. This work provides the foundation for further investigation of these promising novel structures as antiviral agents against Chikungunya virus.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Publisher: Elsevier
ISSN: 0968-0896
Date of First Compliant Deposit: 8 January 2018
Date of Acceptance: 3 January 2018
Last Modified: 15 Mar 2020 01:27

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