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

Andrea Magri; Roisin Reilly; Nicolò Scalacci; Marco Radi; Michael Hunter; Manon Ripoll; Arvind H. Patel; Daniele Castagnolo

doi:10.1016/j.bmcl.2015.09.029

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

Andrea Magri, Roisin Reilly, Nicolò Scalacci, Marco Radi, Michael Hunter, Manon Ripoll, Arvind H. Patel, Daniele Castagnolo

Institute of Pharmaceutical Science

Research output: Contribution to journal › Article › peer-review

30 Citations (Scopus)

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.

Original language	English
Pages (from-to)	5372-5376
Number of pages	5
Journal	Bioorganic & medicinal chemistry letters
Volume	25
Issue number	22
DOIs	https://doi.org/10.1016/j.bmcl.2015.09.029
Publication status	Published - 15 Nov 2015

Keywords

HCV
Amidinourea
Guanidine
Hepatitis C life cycle
RNA replication

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/j.bmcl.2015.09.029

Cite this

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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.",

keywords = "HCV, Amidinourea, Guanidine, Hepatitis C life cycle, RNA replication",

author = "Andrea Magri and Roisin Reilly and Nicol{\`o} Scalacci and Marco Radi and Michael Hunter and Manon Ripoll and Patel, {Arvind H.} and Daniele Castagnolo",

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doi = "10.1016/j.bmcl.2015.09.029",

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T1 - Rethinking the old antiviral drug moroxydine: Discovery of novel analogues as anti-hepatitis C virus (HCV) agents

AU - Magri, Andrea

AU - Reilly, Roisin

AU - Scalacci, Nicolò

AU - Radi, Marco

AU - Hunter, Michael

AU - Ripoll, Manon

AU - Patel, Arvind H.

AU - Castagnolo, Daniele

PY - 2015/11/15

Y1 - 2015/11/15

N2 - 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.

AB - 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.

KW - HCV

KW - Amidinourea

KW - Guanidine

KW - Hepatitis C life cycle

KW - RNA replication

U2 - 10.1016/j.bmcl.2015.09.029

DO - 10.1016/j.bmcl.2015.09.029

M3 - Article

SN - 0960-894X

VL - 25

SP - 5372

EP - 5376

JO - Bioorganic & medicinal chemistry letters

JF - Bioorganic & medicinal chemistry letters

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ER -