title: Rethinking the old antiviral drug moroxydine: Discovery of novel analogues as anti-hepatitis C virus (HCV) agents.
abstract: The discovery of a novel class of HCV inhibitors is described. The new amidinourea compounds were designed as isosteric analogues of the antiviral drug moroxydine. The two derivatives 11g and 11h showed excellent HCV inhibition activity and viability and proved to inhibit a step(s) of the RNA replication. The new compounds have been synthesized in only three synthetic steps from cheap building blocks and in high yields, thus turning to be promising drug candidates in the development of cheaper HCV treatments.
authors.affiliation: MRC-University of Glasgow Centre for Virus Research, Sir Michael Stoker Building, Garscube Campus, 464 Bearsden Road, Glasgow G61 1QH, United Kingdom.
authors.forename: Andrea
authors.initials: A
authors.lastname: Magri
authors.affiliation: Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST Newcastle upon Tyne, United Kingdom.
authors.forename: Roisin
authors.initials: R
authors.lastname: Reilly
authors.affiliation: Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST Newcastle upon Tyne, United Kingdom.
authors.forename: Nicolò
authors.initials: N
authors.lastname: Scalacci
authors.affiliation: P4T Group, Dipartimento di Farmacia, Università degli Studi di Parma, Viale delle Scienze, 27/A, 43124 Parma, Italy.
authors.forename: Marco
authors.initials: M
authors.lastname: Radi
authors.affiliation: Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST Newcastle upon Tyne, United Kingdom.
authors.forename: Michael
authors.initials: M
authors.lastname: Hunter
authors.affiliation: Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST Newcastle upon Tyne, United Kingdom.
authors.forename: Manon
authors.initials: M
authors.lastname: Ripoll
authors.affiliation: MRC-University of Glasgow Centre for Virus Research, Sir Michael Stoker Building, Garscube Campus, 464 Bearsden Road, Glasgow G61 1QH, United Kingdom. Electronic address: arvind.patel@glasgow.ac.uk.
authors.forename: Arvind H
authors.initials: AH
authors.lastname: Patel
authors.affiliation: Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST Newcastle upon Tyne, United Kingdom. Electronic address: daniele.castagnolo@kcl.ac.uk.
authors.forename: Daniele
authors.initials: D
authors.lastname: Castagnolo
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000191:economics* / Q000494:pharmacology*; D001645:Biguanides; D001681:Biological Assay; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery / Q000639:trends; D016174:Hepacivirus / Q000187:drug effects*; D006801:Humans; D050296:Microbial Viability / Q000187:drug effects; D015394:Molecular Structure; D009025:Morpholines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; D001645:Biguanides; D009025:Morpholines; C005267:moroxydine
keywords: Amidinourea; Guanidine; HCV; Hepatitis C life cycle; RNA replication