Rethinking the old antiviral drug moroxydine: Discovery of novel analogues as anti-hepatitis C virus (HCV) agents

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5372-6. doi: 10.1016/j.bmcl.2015.09.029.

Andrea Magri ¹, Roisin Reilly ², Nicolò Scalacci ², Marco Radi ³, Michael Hunter ², Manon Ripoll ², Arvind H Patel ⁴, Daniele Castagnolo ⁵

Affiliations

1 MRC-University of Glasgow Centre for Virus Research, Sir Michael Stoker Building, Garscube Campus, 464 Bearsden Road, Glasgow G61 1QH, United Kingdom.
2 Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST Newcastle upon Tyne, United Kingdom.
3 P4T Group, Dipartimento di Farmacia, Università degli Studi di Parma, Viale delle Scienze, 27/A, 43124 Parma, Italy.
4 MRC-University of Glasgow Centre for Virus Research, Sir Michael Stoker Building, Garscube Campus, 464 Bearsden Road, Glasgow G61 1QH, United Kingdom. Electronic address: [email protected].
5 Northumbria University Newcastle, Department of Applied Sciences, Ellison Building, Ellison Place, NE1 8ST Newcastle upon Tyne, United Kingdom. Electronic address: [email protected].

PMID: 26428870 DOI: 10.1016/j.bmcl.2015.09.029

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.

Keywords

Amidinourea; Guanidine; HCV; Hepatitis C life cycle; RNA replication.

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