Phosphonylmethoxyalkylpurines and -pyrimidines as inhibitors of African swine fever virus replication in vitro
Identifieur interne : 003342 ( Main/Exploration ); précédent : 003341; suivant : 003343Phosphonylmethoxyalkylpurines and -pyrimidines as inhibitors of African swine fever virus replication in vitro
Auteurs : Carmen Gil-Fernández [Espagne] ; Dolores García-Villal N [Espagne] ; Erik De Clercq [Belgique] ; Ivan Rosenberg [Tchécoslovaquie] ; Antonin Hol [Tchécoslovaquie]Source :
- Antiviral Research [ 0166-3542 ] ; 1987.
English descriptors
- KwdEn :
- Teeft :
- African swine fever, African swine fever virus, African swine fever virus replication, Asfv, Asfv replication, Cell cultures, Cell monolayer, Cell monolayers, Cellular proteins, Cellular uptake, Clercq, Crystal violet, Derivative, Growth medium, Immune sera, Inhibitor, Inhibitory effect, Maintenance medium, Neutralizing antibodies, Newborn calf serum, Phosphonoacetic acid, Plaque, Plaque formation, Pmea, Pmedap, Pmemap, Pyrimidine, Pyrimidine derivatives, Replication, Ruiz gonzalvo, Selectivity, Selectivity index, Slmethionine incorporation, Swine, Test compounds, Uptake method, Vero, Vero cell cultures, Vero cells, Viral, Virus, Virus plaques.
Abstract
Summary: Several phosphonylmethoxyalkylpurine and -pyrimidine derivatives related to (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine [(S)-HPMPA] and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) were evaluated as inhibitors of African swine fever virus (ASFV) replication in Vero cells. (S)-HPMPA has previously been shown to inhibit ASFV replication at a minimum inhibitory concentration (MIC) of 0.01 μg/ml with a selectivity index of 15000. Of the new compounds tested, the following emerged as the most potent and selective inhibitors of ASFV replication: the cyclic phosphonate of (S)-HPMPA [(S)-cHPMPA] with an MIC of 0.2 μg/ml and a selectivity index of 2500, the 2,6-diaminopurine analogue of (S)-HPMPA [(S)-HPMPDAP] with an MIC of 0.5 μg/ml and a selectivity index of 1400, and the cytosine [(S)-HPMPC] and guanine [(S)-HPMPG] analogues with an MIC of 1 μg/ml and a selectivity index of 600–700.
Url:
DOI: 10.1016/S0166-3542(87)80005-0
Affiliations:
- Belgique, Espagne, Tchécoslovaquie
- Bohême centrale, Communauté de Madrid, Province du Brabant flamand, Région flamande
- Louvain, Madrid, Prague
- Katholieke Universiteit Leuven
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Le document en format XML
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xml:lang="en"><term>(S)-HPMPA</term><term>(S)-HPMPC</term><term>(S)-HPMPDAP</term><term>(S)-HPMPG</term><term>(S)-cHPMPA</term><term>African swine fever virus</term><term>PMEA</term><term>PMEDAP</term><term>PMEMAP</term><term>Phosphonylmethoxyalkylpurines and -pyrimidines</term></keywords><keywords scheme="Teeft" xml:lang="en"><term>African swine fever</term><term>African swine fever virus</term><term>African swine fever virus replication</term><term>Asfv</term><term>Asfv replication</term><term>Cell cultures</term><term>Cell monolayer</term><term>Cell monolayers</term><term>Cellular proteins</term><term>Cellular uptake</term><term>Clercq</term><term>Crystal violet</term><term>Derivative</term><term>Growth medium</term><term>Immune sera</term><term>Inhibitor</term><term>Inhibitory effect</term><term>Maintenance medium</term><term>Neutralizing antibodies</term><term>Newborn calf serum</term><term>Phosphonoacetic acid</term><term>Plaque</term><term>Plaque formation</term><term>Pmea</term><term>Pmedap</term><term>Pmemap</term><term>Pyrimidine</term><term>Pyrimidine derivatives</term><term>Replication</term><term>Ruiz gonzalvo</term><term>Selectivity</term><term>Selectivity index</term><term>Slmethionine incorporation</term><term>Swine</term><term>Test compounds</term><term>Uptake method</term><term>Vero</term><term>Vero cell cultures</term><term>Vero cells</term><term>Viral</term><term>Virus</term><term>Virus plaques</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Summary: Several phosphonylmethoxyalkylpurine and -pyrimidine derivatives related to (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine [(S)-HPMPA] and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) were evaluated as inhibitors of African swine fever virus (ASFV) replication in Vero cells. (S)-HPMPA has previously been shown to inhibit ASFV replication at a minimum inhibitory concentration (MIC) of 0.01 μg/ml with a selectivity index of 15000. Of the new compounds tested, the following emerged as the most potent and selective inhibitors of ASFV replication: the cyclic phosphonate of (S)-HPMPA [(S)-cHPMPA] with an MIC of 0.2 μg/ml and a selectivity index of 2500, the 2,6-diaminopurine analogue of (S)-HPMPA [(S)-HPMPDAP] with an MIC of 0.5 μg/ml and a selectivity index of 1400, and the cytosine [(S)-HPMPC] and guanine [(S)-HPMPG] analogues with an MIC of 1 μg/ml and a selectivity index of 600–700.</div></front></TEI><affiliations><list><country><li>Belgique</li><li>Espagne</li><li>Tchécoslovaquie</li></country><region><li>Bohême centrale</li><li>Communauté de Madrid</li><li>Province du Brabant flamand</li><li>Région flamande</li></region><settlement><li>Louvain</li><li>Madrid</li><li>Prague</li></settlement><orgName><li>Katholieke Universiteit Leuven</li></orgName></list><tree><country name="Espagne"><region name="Communauté de Madrid"><name sortKey="Gil Fernandez, Carmen" sort="Gil Fernandez, Carmen" uniqKey="Gil Fernandez C" first="Carmen" last="Gil-Fernández">Carmen Gil-Fernández</name></region><name sortKey="Garcia Villal N, Dolores" sort="Garcia Villal N, Dolores" uniqKey="Garcia Villal N D" first="Dolores" last="García-Villal N">Dolores García-Villal N</name><name sortKey="Gil Fernandez, Carmen" sort="Gil Fernandez, Carmen" uniqKey="Gil Fernandez C" first="Carmen" last="Gil-Fernández">Carmen Gil-Fernández</name></country><country name="Belgique"><region name="Région flamande"><name sortKey="Clercq, Erik De" sort="Clercq, Erik De" uniqKey="Clercq E" first="Erik De" last="Clercq">Erik De Clercq</name></region></country><country name="Tchécoslovaquie"><region name="Bohême centrale"><name sortKey="Rosenberg, Ivan" sort="Rosenberg, Ivan" uniqKey="Rosenberg I" first="Ivan" last="Rosenberg">Ivan Rosenberg</name></region><name sortKey="Hol, Antonin" sort="Hol, Antonin" uniqKey="Hol A" first="Antonin" last="Hol">Antonin Hol</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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