Design, Synthesis and Biological Evaluation of Novel Piperazine Derivatives as CCR5 Antagonists
Identifieur interne : 001966 ( Main/Exploration ); précédent : 001965; suivant : 001967Design, Synthesis and Biological Evaluation of Novel Piperazine Derivatives as CCR5 Antagonists
Auteurs : Tao Liu [République populaire de Chine] ; Zhiyong Weng [République populaire de Chine] ; Xiaowu Dong [République populaire de Chine] ; Linjie Chen [République populaire de Chine] ; Ling Ma [République populaire de Chine] ; Shan Cen [République populaire de Chine] ; Naiming Zhou [République populaire de Chine] ; Yongzhou Hu [République populaire de Chine]Source :
- PLoS ONE [ 1932-6203 ] ; 2013.
Descripteurs français
- KwdFr :
- Agents antiVIH (pharmacologie), Agents antiVIH (synthèse chimique), Antagonistes des récepteurs CCR5, Cellules HEK293, Concentration inhibitrice 50, Conception de médicament, Dosage biologique, Expression des gènes, Fusion cellulaire, Gènes rapporteurs, Humains, Luciferases, Pipérazines (pharmacologie), Pipérazines (synthèse chimique), Protéine d'enveloppe gp120 du VIH (génétique), Protéine d'enveloppe gp120 du VIH (métabolisme), Relation structure-activité, Récepteurs CCR5 (métabolisme), Survie cellulaire (), VIH-1 (Virus de l'Immunodéficience Humaine de type 1) (), VIH-1 (Virus de l'Immunodéficience Humaine de type 1) (croissance et développement).
- MESH :
- croissance et développement : VIH-1 (Virus de l'Immunodéficience Humaine de type 1).
- génétique : Protéine d'enveloppe gp120 du VIH.
- métabolisme : Protéine d'enveloppe gp120 du VIH, Récepteurs CCR5.
- pharmacologie : Agents antiVIH, Pipérazines.
- synthèse chimique : Agents antiVIH, Pipérazines.
- Antagonistes des récepteurs CCR5, Cellules HEK293, Concentration inhibitrice 50, Conception de médicament, Dosage biologique, Expression des gènes, Fusion cellulaire, Gènes rapporteurs, Humains, Luciferases, Relation structure-activité, Survie cellulaire, VIH-1 (Virus de l'Immunodéficience Humaine de type 1).
English descriptors
- KwdEn :
- Anti-HIV Agents (chemical synthesis), Anti-HIV Agents (pharmacology), Biological Assay, CCR5 Receptor Antagonists, CD4 Antigens (genetics), CD4 Antigens (metabolism), Cell Fusion, Cell Survival (drug effects), Drug Design, Gene Expression, Genes, Reporter, HEK293 Cells, HIV Envelope Protein gp120 (genetics), HIV Envelope Protein gp120 (metabolism), HIV-1 (drug effects), HIV-1 (growth & development), Humans, Inhibitory Concentration 50, Luciferases, Piperazines (chemical synthesis), Piperazines (pharmacology), Receptors, CCR5 (metabolism), Structure-Activity Relationship.
- MESH :
- chemical , chemical synthesis : Anti-HIV Agents, Piperazines.
- chemical , genetics : CD4 Antigens, HIV Envelope Protein gp120.
- chemical , metabolism : CD4 Antigens, HIV Envelope Protein gp120, Receptors, CCR5.
- chemical , pharmacology : Anti-HIV Agents, Piperazines.
- drug effects : Cell Survival, HIV-1.
- growth & development : HIV-1.
- Biological Assay, CCR5 Receptor Antagonists, Cell Fusion, Drug Design, Gene Expression, Genes, Reporter, HEK293 Cells, Humans, Inhibitory Concentration 50, Luciferases, Structure-Activity Relationship.
Abstract
By using a fragment-assembly strategy and bioisosteric-replacement principle, a series of novel piperazine derivatives were designed, synthesized, and evaluated for their cellular target-effector fusion activities and in vitro antiviral activities against HIV-1. Preliminary structure-activity relationships (SARs) of target compounds were concluded in this study, and five compounds were found to exhibited medium to potent CCR5 fusion activities with IC50 values in low micromolar level. Among evaluated compounds,
Url:
DOI: 10.1371/journal.pone.0053636
PubMed: 23308267
PubMed Central: 3538727
Affiliations:
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Le document en format XML
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of Novel Piperazine Derivatives as CCR5 Antagonists</title><author><name sortKey="Liu, Tao" sort="Liu, Tao" uniqKey="Liu T" first="Tao" last="Liu">Tao Liu</name><affiliation wicri:level="3"><nlm:aff id="aff1"><addr-line>Zhejiang University-École Normale Supérieure Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Zhejiang University-École Normale Supérieure Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou</wicri:regionArea><placeName><settlement type="city">Hangzhou</settlement><region type="province">Zhejiang</region></placeName></affiliation></author><author><name sortKey="Weng, Zhiyong" sort="Weng, Zhiyong" uniqKey="Weng Z" first="Zhiyong" last="Weng">Zhiyong Weng</name><affiliation wicri:level="3"><nlm:aff id="aff1"><addr-line>Zhejiang University-École Normale Supérieure Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Zhejiang University-École Normale Supérieure Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou</wicri:regionArea><placeName><settlement type="city">Hangzhou</settlement><region type="province">Zhejiang</region></placeName></affiliation></author><author><name sortKey="Dong, Xiaowu" sort="Dong, Xiaowu" uniqKey="Dong X" first="Xiaowu" last="Dong">Xiaowu Dong</name><affiliation wicri:level="3"><nlm:aff id="aff1"><addr-line>Zhejiang University-École Normale Supérieure Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Zhejiang University-École Normale Supérieure Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou</wicri:regionArea><placeName><settlement type="city">Hangzhou</settlement><region type="province">Zhejiang</region></placeName></affiliation></author><author><name sortKey="Chen, Linjie" sort="Chen, Linjie" uniqKey="Chen L" first="Linjie" last="Chen">Linjie Chen</name><affiliation wicri:level="4"><nlm:aff id="aff2"><addr-line>Institute of Biochemistry, College of Life Sciences, Zhejiang University, Hangzhou, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Institute of Biochemistry, College of Life Sciences, Zhejiang University, Hangzhou</wicri:regionArea><placeName><settlement type="city">Hangzhou</settlement><region type="province">Zhejiang</region></placeName><orgName type="university">Université de Zhejiang</orgName></affiliation></author><author><name sortKey="Ma, Ling" sort="Ma, Ling" uniqKey="Ma L" first="Ling" last="Ma">Ling Ma</name><affiliation wicri:level="3"><nlm:aff id="aff3"><addr-line>Insititute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Beijing, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Insititute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Beijing</wicri:regionArea><placeName><settlement type="city">Pékin</settlement></placeName></affiliation><affiliation wicri:level="3"><nlm:aff id="aff4"><addr-line>Peking Union Medical College, Beijing, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Peking Union Medical College, Beijing</wicri:regionArea><placeName><settlement type="city">Pékin</settlement></placeName></affiliation></author><author><name sortKey="Cen, Shan" sort="Cen, Shan" uniqKey="Cen S" first="Shan" last="Cen">Shan Cen</name><affiliation wicri:level="3"><nlm:aff id="aff3"><addr-line>Insititute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Beijing, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Insititute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Beijing</wicri:regionArea><placeName><settlement type="city">Pékin</settlement></placeName></affiliation><affiliation wicri:level="3"><nlm:aff id="aff4"><addr-line>Peking Union Medical College, Beijing, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Peking Union Medical College, Beijing</wicri:regionArea><placeName><settlement type="city">Pékin</settlement></placeName></affiliation></author><author><name sortKey="Zhou, Naiming" sort="Zhou, Naiming" uniqKey="Zhou N" first="Naiming" last="Zhou">Naiming Zhou</name><affiliation wicri:level="4"><nlm:aff id="aff2"><addr-line>Institute of Biochemistry, College of Life Sciences, Zhejiang University, Hangzhou, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Institute of Biochemistry, College of Life Sciences, Zhejiang University, Hangzhou</wicri:regionArea><placeName><settlement type="city">Hangzhou</settlement><region type="province">Zhejiang</region></placeName><orgName type="university">Université de Zhejiang</orgName></affiliation></author><author><name sortKey="Hu, Yongzhou" sort="Hu, Yongzhou" uniqKey="Hu Y" first="Yongzhou" last="Hu">Yongzhou Hu</name><affiliation wicri:level="3"><nlm:aff id="aff1"><addr-line>Zhejiang University-École Normale Supérieure Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China</addr-line></nlm:aff><country xml:lang="fr">République populaire de Chine</country><wicri:regionArea>Zhejiang University-École Normale Supérieure Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou</wicri:regionArea><placeName><settlement type="city">Hangzhou</settlement><region type="province">Zhejiang</region></placeName></affiliation></author></analytic><series><title level="j">PLoS ONE</title><idno type="eISSN">1932-6203</idno><imprint><date when="2013">2013</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Anti-HIV Agents (chemical synthesis)</term><term>Anti-HIV Agents (pharmacology)</term><term>Biological Assay</term><term>CCR5 Receptor Antagonists</term><term>CD4 Antigens (genetics)</term><term>CD4 Antigens (metabolism)</term><term>Cell Fusion</term><term>Cell Survival (drug effects)</term><term>Drug Design</term><term>Gene Expression</term><term>Genes, Reporter</term><term>HEK293 Cells</term><term>HIV Envelope Protein gp120 (genetics)</term><term>HIV Envelope Protein gp120 (metabolism)</term><term>HIV-1 (drug effects)</term><term>HIV-1 (growth & development)</term><term>Humans</term><term>Inhibitory Concentration 50</term><term>Luciferases</term><term>Piperazines (chemical synthesis)</term><term>Piperazines (pharmacology)</term><term>Receptors, CCR5 (metabolism)</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Agents antiVIH (pharmacologie)</term><term>Agents antiVIH (synthèse chimique)</term><term>Antagonistes des récepteurs CCR5</term><term>Cellules HEK293</term><term>Concentration inhibitrice 50</term><term>Conception de médicament</term><term>Dosage biologique</term><term>Expression des gènes</term><term>Fusion cellulaire</term><term>Gènes rapporteurs</term><term>Humains</term><term>Luciferases</term><term>Pipérazines (pharmacologie)</term><term>Pipérazines (synthèse chimique)</term><term>Protéine d'enveloppe gp120 du VIH (génétique)</term><term>Protéine d'enveloppe gp120 du VIH (métabolisme)</term><term>Relation structure-activité</term><term>Récepteurs CCR5 (métabolisme)</term><term>Survie cellulaire ()</term><term>VIH-1 (Virus de l'Immunodéficience Humaine de type 1) ()</term><term>VIH-1 (Virus de l'Immunodéficience Humaine de type 1) (croissance et développement)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Anti-HIV Agents</term><term>Piperazines</term></keywords><keywords scheme="MESH" type="chemical" qualifier="genetics" xml:lang="en"><term>CD4 Antigens</term><term>HIV Envelope Protein gp120</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>CD4 Antigens</term><term>HIV Envelope Protein gp120</term><term>Receptors, CCR5</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Anti-HIV Agents</term><term>Piperazines</term></keywords><keywords scheme="MESH" qualifier="croissance et développement" xml:lang="fr"><term>VIH-1 (Virus de l'Immunodéficience Humaine de type 1)</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Cell Survival</term><term>HIV-1</term></keywords><keywords scheme="MESH" qualifier="growth & development" xml:lang="en"><term>HIV-1</term></keywords><keywords scheme="MESH" qualifier="génétique" xml:lang="fr"><term>Protéine d'enveloppe gp120 du VIH</term></keywords><keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Protéine d'enveloppe gp120 du VIH</term><term>Récepteurs CCR5</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Agents antiVIH</term><term>Pipérazines</term></keywords><keywords scheme="MESH" qualifier="synthèse chimique" xml:lang="fr"><term>Agents antiVIH</term><term>Pipérazines</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Biological Assay</term><term>CCR5 Receptor Antagonists</term><term>Cell Fusion</term><term>Drug Design</term><term>Gene Expression</term><term>Genes, Reporter</term><term>HEK293 Cells</term><term>Humans</term><term>Inhibitory Concentration 50</term><term>Luciferases</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Antagonistes des récepteurs CCR5</term><term>Cellules HEK293</term><term>Concentration inhibitrice 50</term><term>Conception de médicament</term><term>Dosage biologique</term><term>Expression des gènes</term><term>Fusion cellulaire</term><term>Gènes rapporteurs</term><term>Humains</term><term>Luciferases</term><term>Relation structure-activité</term><term>Survie cellulaire</term><term>VIH-1 (Virus de l'Immunodéficience Humaine de type 1)</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en"><p>By using a fragment-assembly strategy and bioisosteric-replacement principle, a series of novel piperazine derivatives were designed, synthesized, and evaluated for their cellular target-effector fusion activities and in vitro antiviral activities against HIV-1. Preliminary structure-activity relationships (SARs) of target compounds were concluded in this study, and five compounds were found to exhibited medium to potent CCR5 fusion activities with IC<sub>50</sub> values in low micromolar level. Among evaluated compounds, <bold>23 h</bold> was found to be a CCR5 antagonist with an IC<sub>50</sub> value of 6.29 µM and an anti-HIV-1 inhibitor with an IC<sub>50</sub> value of 0.44 µM.</p></div></front><back><div1 type="bibliography"><listBibl><biblStruct><analytic><author><name sortKey="Yerly, S" uniqKey="Yerly S">S Yerly</name></author><author><name sortKey="Kaiser, L" uniqKey="Kaiser L">L Kaiser</name></author><author><name sortKey="Race, E" uniqKey="Race E">E Race</name></author><author><name sortKey="Bru, Jp" uniqKey="Bru J">JP Bru</name></author><author><name sortKey="Clavel, F" uniqKey="Clavel F">F Clavel</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Combadiere, C" uniqKey="Combadiere C">C Combadiere</name></author><author><name sortKey="Ahuja, Sk" uniqKey="Ahuja S">SK Ahuja</name></author><author><name sortKey="Tiffany, Hl" uniqKey="Tiffany H">HL Tiffany</name></author><author><name sortKey="Murphy, Pm" uniqKey="Murphy P">PM Murphy</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Deng, H" uniqKey="Deng H">H Deng</name></author><author><name sortKey="Liu, R" uniqKey="Liu R">R Liu</name></author><author><name sortKey="Ellmeier, W" uniqKey="Ellmeier W">W Ellmeier</name></author><author><name sortKey="Choe, S" uniqKey="Choe S">S Choe</name></author><author><name sortKey="Unutmaz, D" uniqKey="Unutmaz D">D Unutmaz</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Rodger, Dm" uniqKey="Rodger D">DM Rodger</name></author><author><name sortKey="Richard, Mn" uniqKey="Richard M">MN Richard</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Takashima, K" uniqKey="Takashima K">K Takashima</name></author><author><name sortKey="Miyake, H" uniqKey="Miyake H">H Miyake</name></author><author><name sortKey="Kanzaki, N" uniqKey="Kanzaki N">N Kanzaki</name></author><author><name sortKey="Tagawa, Y" uniqKey="Tagawa Y">Y Tagawa</name></author><author><name sortKey="Wang, X" uniqKey="Wang X">X Wang</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Nishikawa, M" uniqKey="Nishikawa M">M Nishikawa</name></author><author><name sortKey="Takashima, K" uniqKey="Takashima K">K Takashima</name></author><author><name sortKey="Nishi, T" uniqKey="Nishi T">T Nishi</name></author><author><name sortKey="Furuta, Ra" uniqKey="Furuta R">RA Furuta</name></author><author><name sortKey="Kanzaki, N" uniqKey="Kanzaki N">N Kanzaki</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Kondru, R" uniqKey="Kondru R">R Kondru</name></author><author><name sortKey="Zhang, J" uniqKey="Zhang J">J Zhang</name></author><author><name sortKey="Ji, Ch" uniqKey="Ji C">CH Ji</name></author><author><name sortKey="Mirzadegan, T" uniqKey="Mirzadegan T">T Mirzadegan</name></author><author><name sortKey="Rotstein, D" uniqKey="Rotstein D">D Rotstein</name></author></analytic></biblStruct><biblStruct></biblStruct><biblStruct><analytic><author><name sortKey="Feng, Dz" uniqKey="Feng D">DZ Feng</name></author><author><name sortKey="Song, Yl" uniqKey="Song Y">YL Song</name></author><author><name sortKey="Jiang, Xh" uniqKey="Jiang X">XH Jiang</name></author><author><name sortKey="Chen, L" uniqKey="Chen L">L Chen</name></author><author><name sortKey="Long, Yq" uniqKey="Long Y">YQ Long</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Jiang, Xh" uniqKey="Jiang X">XH Jiang</name></author><author><name sortKey="Song, Yl" uniqKey="Song Y">YL Song</name></author><author><name sortKey="Long, Yq" uniqKey="Long Y">YQ Long</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Torre, O" uniqKey="Torre O">O Torre</name></author><author><name sortKey="Gotor Fernandez, V" uniqKey="Gotor Fernandez V">V Gotor-Fernández</name></author><author><name sortKey="Gotor, V" uniqKey="Gotor V">V Gotor</name></author></analytic></biblStruct><biblStruct></biblStruct><biblStruct><analytic><author><name sortKey="Chen, Lj" uniqKey="Chen L">LJ Chen</name></author><author><name sortKey="Zhang, Yp" uniqKey="Zhang Y">YP Zhang</name></author><author><name sortKey="Li, G" uniqKey="Li G">G Li</name></author><author><name sortKey="Huang, Hs" uniqKey="Huang H">HS Huang</name></author><author><name sortKey="Zhou, Nm" uniqKey="Zhou N">NM Zhou</name></author></analytic></biblStruct><biblStruct><analytic><author><name sortKey="Coakley, E" uniqKey="Coakley E">E Coakley</name></author><author><name sortKey="Petropoulos, C" uniqKey="Petropoulos C">C Petropoulos</name></author><author><name sortKey="Whitcomb, J" uniqKey="Whitcomb J">J Whitcomb</name></author></analytic></biblStruct></listBibl></div1></back></TEI><affiliations><list><country><li>République populaire de Chine</li></country><region><li>Zhejiang</li></region><settlement><li>Hangzhou</li><li>Pékin</li></settlement><orgName><li>Université de Zhejiang</li></orgName></list><tree><country name="République populaire de Chine"><region name="Zhejiang"><name sortKey="Liu, Tao" sort="Liu, Tao" uniqKey="Liu T" first="Tao" last="Liu">Tao Liu</name></region><name sortKey="Cen, Shan" sort="Cen, Shan" uniqKey="Cen S" first="Shan" last="Cen">Shan Cen</name><name sortKey="Cen, Shan" sort="Cen, Shan" uniqKey="Cen S" first="Shan" last="Cen">Shan Cen</name><name sortKey="Chen, Linjie" sort="Chen, Linjie" uniqKey="Chen L" first="Linjie" last="Chen">Linjie Chen</name><name sortKey="Dong, Xiaowu" sort="Dong, Xiaowu" uniqKey="Dong X" first="Xiaowu" last="Dong">Xiaowu Dong</name><name sortKey="Hu, Yongzhou" sort="Hu, Yongzhou" uniqKey="Hu Y" first="Yongzhou" last="Hu">Yongzhou Hu</name><name sortKey="Ma, Ling" sort="Ma, Ling" uniqKey="Ma L" first="Ling" last="Ma">Ling Ma</name><name sortKey="Ma, Ling" sort="Ma, Ling" uniqKey="Ma L" first="Ling" last="Ma">Ling Ma</name><name sortKey="Weng, Zhiyong" sort="Weng, Zhiyong" uniqKey="Weng Z" first="Zhiyong" last="Weng">Zhiyong Weng</name><name sortKey="Zhou, Naiming" sort="Zhou, Naiming" uniqKey="Zhou N" first="Naiming" last="Zhou">Naiming Zhou</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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