Quantitative structure-activity relationships (QSARs) of pyrimidine nucleosides as HIV-1 antiviral agents.
Identifieur interne : 002073 ( Ncbi/Checkpoint ); précédent : 002072; suivant : 002074Quantitative structure-activity relationships (QSARs) of pyrimidine nucleosides as HIV-1 antiviral agents.
Auteurs : M. MahmoudianSource :
- Pharmaceutical research [ 0724-8741 ] ; 1991.
Descripteurs français
- KwdFr :
- MESH :
- pharmacologie : Antiviraux, Nucléosides pyrimidiques.
- synthèse chimique : Antiviraux, Nucléosides pyrimidiques.
- Nucléosides pyrimidiques, Relation structure-activité, VIH-1 (Virus de l'Immunodéficience Humaine de type 1).
English descriptors
- KwdEn :
- MESH :
- chemical , chemical synthesis : Antiviral Agents, Pyrimidine Nucleosides.
- chemical , chemistry : Pyrimidine Nucleosides.
- chemical , pharmacology : Antiviral Agents, Pyrimidine Nucleosides.
- drug effects : HIV-1.
- Structure-Activity Relationship.
Abstract
The structural requirements for the antiviral activity of pyrimidine nucleosides against HIV-1 virus was evaluated with the Hansch SAR analysis. Antiviral activity is best related to the hydrophobicity and steric (L and B3) properties of the substituent at the C5 of pyrimidine ring. Further, the antiviral activity is related to B4 of the substituent at position 3' of the sugar ring with a positive slope. The activity of both uracil and cytosine derivatives can be related to their structure by the same equations, which indicates that the SARs are similar in these two groups of congeners. These results suggest that compounds with a small substituent at the 5 position of the pyrimidine ring and a flat substituent at the 3' position of the sugar ring will be the most active compounds against HIV-1 virus.
DOI: 10.1023/a:1015822105022
PubMed: 2014207
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream PubMed, to step Corpus: 003556
- to stream PubMed, to step Curation: 003556
- to stream PubMed, to step Checkpoint: 003443
- to stream Ncbi, to step Merge: 002073
- to stream Ncbi, to step Curation: 002073
Links to Exploration step
pubmed:2014207Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Quantitative structure-activity relationships (QSARs) of pyrimidine nucleosides as HIV-1 antiviral agents.</title>
<author><name sortKey="Mahmoudian, M" sort="Mahmoudian, M" uniqKey="Mahmoudian M" first="M" last="Mahmoudian">M. Mahmoudian</name>
<affiliation><nlm:affiliation>Department of Pharmacology, University of Medical Sciences of Iran Firoozgar Institute, Tehran.</nlm:affiliation>
<wicri:noCountry code="subField">Tehran</wicri:noCountry>
</affiliation>
</author>
</titleStmt>
<publicationStmt><idno type="wicri:source">PubMed</idno>
<date when="1991">1991</date>
<idno type="RBID">pubmed:2014207</idno>
<idno type="pmid">2014207</idno>
<idno type="doi">10.1023/a:1015822105022</idno>
<idno type="wicri:Area/PubMed/Corpus">003556</idno>
<idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">003556</idno>
<idno type="wicri:Area/PubMed/Curation">003556</idno>
<idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">003556</idno>
<idno type="wicri:Area/PubMed/Checkpoint">003443</idno>
<idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">003443</idno>
<idno type="wicri:Area/Ncbi/Merge">002073</idno>
<idno type="wicri:Area/Ncbi/Curation">002073</idno>
<idno type="wicri:Area/Ncbi/Checkpoint">002073</idno>
</publicationStmt>
<sourceDesc><biblStruct><analytic><title xml:lang="en">Quantitative structure-activity relationships (QSARs) of pyrimidine nucleosides as HIV-1 antiviral agents.</title>
<author><name sortKey="Mahmoudian, M" sort="Mahmoudian, M" uniqKey="Mahmoudian M" first="M" last="Mahmoudian">M. Mahmoudian</name>
<affiliation><nlm:affiliation>Department of Pharmacology, University of Medical Sciences of Iran Firoozgar Institute, Tehran.</nlm:affiliation>
<wicri:noCountry code="subField">Tehran</wicri:noCountry>
</affiliation>
</author>
</analytic>
<series><title level="j">Pharmaceutical research</title>
<idno type="ISSN">0724-8741</idno>
<imprint><date when="1991" type="published">1991</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antiviral Agents (chemical synthesis)</term>
<term>Antiviral Agents (pharmacology)</term>
<term>HIV-1 (drug effects)</term>
<term>Pyrimidine Nucleosides (chemical synthesis)</term>
<term>Pyrimidine Nucleosides (chemistry)</term>
<term>Pyrimidine Nucleosides (pharmacology)</term>
<term>Structure-Activity Relationship</term>
</keywords>
<keywords scheme="KwdFr" xml:lang="fr"><term>Antiviraux (pharmacologie)</term>
<term>Antiviraux (synthèse chimique)</term>
<term>Nucléosides pyrimidiques ()</term>
<term>Nucléosides pyrimidiques (pharmacologie)</term>
<term>Nucléosides pyrimidiques (synthèse chimique)</term>
<term>Relation structure-activité</term>
<term>VIH-1 (Virus de l'Immunodéficience Humaine de type 1) ()</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Antiviral Agents</term>
<term>Pyrimidine Nucleosides</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Pyrimidine Nucleosides</term>
</keywords>
<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term>
<term>Pyrimidine Nucleosides</term>
</keywords>
<keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>HIV-1</term>
</keywords>
<keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term>
<term>Nucléosides pyrimidiques</term>
</keywords>
<keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Antiviraux</term>
<term>Nucléosides pyrimidiques</term>
</keywords>
<keywords scheme="MESH" xml:lang="en"><term>Structure-Activity Relationship</term>
</keywords>
<keywords scheme="MESH" xml:lang="fr"><term>Nucléosides pyrimidiques</term>
<term>Relation structure-activité</term>
<term>VIH-1 (Virus de l'Immunodéficience Humaine de type 1)</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">The structural requirements for the antiviral activity of pyrimidine nucleosides against HIV-1 virus was evaluated with the Hansch SAR analysis. Antiviral activity is best related to the hydrophobicity and steric (L and B3) properties of the substituent at the C5 of pyrimidine ring. Further, the antiviral activity is related to B4 of the substituent at position 3' of the sugar ring with a positive slope. The activity of both uracil and cytosine derivatives can be related to their structure by the same equations, which indicates that the SARs are similar in these two groups of congeners. These results suggest that compounds with a small substituent at the 5 position of the pyrimidine ring and a flat substituent at the 3' position of the sugar ring will be the most active compounds against HIV-1 virus.</div>
</front>
</TEI>
<affiliations><list></list>
<tree><noCountry><name sortKey="Mahmoudian, M" sort="Mahmoudian, M" uniqKey="Mahmoudian M" first="M" last="Mahmoudian">M. Mahmoudian</name>
</noCountry>
</tree>
</affiliations>
</record>
Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/SrasV1/Data/Ncbi/Checkpoint
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 002073 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Ncbi/Checkpoint/biblio.hfd -nk 002073 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien |wiki= Sante |area= SrasV1 |flux= Ncbi |étape= Checkpoint |type= RBID |clé= pubmed:2014207 |texte= Quantitative structure-activity relationships (QSARs) of pyrimidine nucleosides as HIV-1 antiviral agents. }}
Pour générer des pages wiki
HfdIndexSelect -h $EXPLOR_AREA/Data/Ncbi/Checkpoint/RBID.i -Sk "pubmed:2014207" \ | HfdSelect -Kh $EXPLOR_AREA/Data/Ncbi/Checkpoint/biblio.hfd \ | NlmPubMed2Wicri -a SrasV1
This area was generated with Dilib version V0.6.33. |