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Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus

Giancotti, Gilda, Cancellieri, Michela, Balboni, Andrea, Giustiniano, Mariateresa, Novellino, Ettore, Delang, Leen, Neyts, Johan, Leyssen, Pieter, Brancale, Andrea and Bassetto, Marcella 2018. Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus. European Journal of Medicinal Chemistry 149 , pp. 56-68. 10.1016/j.ejmech.2018.02.054

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Abstract

Chikungunya virus is a re-emerging arbovirus transmitted to humans by Aedes mosquitoes, responsible for an acute febrile illness associated with painful and debilitating arthralgia, which can persist for several months or become chronic. Over the past few years, infection with this virus has spread worldwide with a previously unknown virulence. No specific antiviral treatments nor vaccines are currently available against this important pathogen. Starting from the structure of a class of selective anti-CHIKV agents previously identified in our research group, different modifications to this scaffold were rationally designed, and 69 novel small-molecule derivatives were synthesised and evaluated for their inhibition of Chikungunya virus replication in Vero cells. Further structure-activity relationships associated with this class of antiviral agents were elucidated for the original scaffolds, and novel antiviral compounds with EC50 values in the low micromolar range were identified. This work provides the foundation for further investigation of these new structures as antivirals against Chikungunya virus.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Publisher: Elsevier
ISSN: 0223-5234
Date of First Compliant Deposit: 26 February 2018
Date of Acceptance: 16 February 2018
Last Modified: 03 Jul 2019 06:24
URI: http://orca-mwe.cf.ac.uk/id/eprint/109500

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