Functionalized triazines as potent HCV entry inhibitors.
Identifieur interne : 000E29 ( Main/Exploration ); précédent : 000E28; suivant : 000E30Functionalized triazines as potent HCV entry inhibitors.
Auteurs : Eric S. Mull [États-Unis] ; Li-Qiang Sun [États-Unis] ; Qian Zhao [États-Unis] ; Betsy Eggers [États-Unis] ; Kevin Pokornowski [États-Unis] ; Guangzhi Zhai [États-Unis] ; Ramkumar Rajamani [États-Unis] ; Susan Jenkins [États-Unis] ; Melissa Kramer [États-Unis] ; Ying-Kai Wang [États-Unis] ; Hua Fang [États-Unis] ; Daniel Tenney [États-Unis] ; Carl J. Baldick [États-Unis] ; Mark I. Cockett [États-Unis] ; Nicholas A. Meanwell [États-Unis] ; Paul M. Scola [États-Unis]Source :
- Bioorganic & medicinal chemistry letters [ 1464-3405 ] ; 2017.
Descripteurs français
- KwdFr :
- MESH :
- pharmacocinétique : Antiviraux, Triazines.
- pharmacologie : Antiviraux, Triazines.
- physiologie : Hepacivirus.
- Animaux, Antiviraux, Fusion membranaire, Hepacivirus, Humains, Rats, Relation structure-activité, Triazines.
English descriptors
- KwdEn :
- Animals, Antiviral Agents (chemistry), Antiviral Agents (pharmacokinetics), Antiviral Agents (pharmacology), Hepacivirus (drug effects), Hepacivirus (physiology), Humans, Membrane Fusion (drug effects), Rats, Structure-Activity Relationship, Triazines (chemistry), Triazines (pharmacokinetics), Triazines (pharmacology).
- MESH :
- chemical , chemistry : Antiviral Agents, Triazines.
- chemical , pharmacokinetics : Antiviral Agents, Triazines.
- chemical , pharmacology : Antiviral Agents, Triazines.
- drug effects : Hepacivirus, Membrane Fusion.
- physiology : Hepacivirus.
- Animals, Humans, Rats, Structure-Activity Relationship.
Abstract
A series of potent and novel acylsulfonamide-bearing triazines were synthesized and the structure-activity relationships (SARs) as HCV entry inhibitors were evaluated. This acylsulfonamide series was derived from an early lead, 4-(4-(1-(4-chlorophenyl)cyclopropylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)benzoic acid wherein the carboxylic acid was replaced with an acylsulfonamide moiety. This structural modification provided a class of compounds which projected an additional vector off the terminus of the acylsulfonamide functionality as a means to drive activity. This effort led to the discovery of potent analogues within this series that demonstrated sub-nanomolar EC50 values in the HCV pseudotype particle (HCVpp) assay.
DOI: 10.1016/j.bmcl.2016.12.038
PubMed: 28089701
Affiliations:
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Mull</name><affiliation wicri:level="2"><nlm:affiliation>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States. Electronic address: eric_mull@hotmail.com.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Sun, Li Qiang" sort="Sun, Li Qiang" uniqKey="Sun L" first="Li-Qiang" last="Sun">Li-Qiang Sun</name><affiliation wicri:level="2"><nlm:affiliation>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Zhao, Qian" sort="Zhao, Qian" uniqKey="Zhao Q" first="Qian" last="Zhao">Qian Zhao</name><affiliation wicri:level="2"><nlm:affiliation>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Eggers, Betsy" sort="Eggers, Betsy" uniqKey="Eggers B" first="Betsy" last="Eggers">Betsy Eggers</name><affiliation wicri:level="2"><nlm:affiliation>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Pokornowski, Kevin" sort="Pokornowski, Kevin" uniqKey="Pokornowski K" first="Kevin" last="Pokornowski">Kevin Pokornowski</name><affiliation wicri:level="2"><nlm:affiliation>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Zhai, Guangzhi" sort="Zhai, Guangzhi" uniqKey="Zhai G" first="Guangzhi" last="Zhai">Guangzhi Zhai</name><affiliation wicri:level="2"><nlm:affiliation>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Rajamani, Ramkumar" sort="Rajamani, Ramkumar" uniqKey="Rajamani R" first="Ramkumar" last="Rajamani">Ramkumar Rajamani</name><affiliation wicri:level="2"><nlm:affiliation>Department of Computer-Assisted Drug Design, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Computer-Assisted Drug Design, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Jenkins, Susan" sort="Jenkins, Susan" uniqKey="Jenkins S" first="Susan" last="Jenkins">Susan Jenkins</name><affiliation wicri:level="2"><nlm:affiliation>Department of Pharmaceutical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmaceutical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Kramer, Melissa" sort="Kramer, Melissa" uniqKey="Kramer M" first="Melissa" last="Kramer">Melissa Kramer</name><affiliation wicri:level="2"><nlm:affiliation>Department of Pharmaceutical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Pharmaceutical Candidate Optimization, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Wang, Ying Kai" sort="Wang, Ying Kai" uniqKey="Wang Y" first="Ying-Kai" last="Wang">Ying-Kai Wang</name><affiliation wicri:level="2"><nlm:affiliation>Department of Lead Evaluation, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Lead Evaluation, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Fang, Hua" sort="Fang, Hua" uniqKey="Fang H" first="Hua" last="Fang">Hua Fang</name><affiliation wicri:level="2"><nlm:affiliation>Department of Lead Evaluation, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Lead Evaluation, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Tenney, Daniel" sort="Tenney, Daniel" uniqKey="Tenney D" first="Daniel" last="Tenney">Daniel Tenney</name><affiliation wicri:level="2"><nlm:affiliation>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Baldick, Carl J" sort="Baldick, Carl J" uniqKey="Baldick C" first="Carl J" last="Baldick">Carl J. Baldick</name><affiliation wicri:level="2"><nlm:affiliation>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Cockett, Mark I" sort="Cockett, Mark I" uniqKey="Cockett M" first="Mark I" last="Cockett">Mark I. Cockett</name><affiliation wicri:level="2"><nlm:affiliation>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Virology Discovery Biology, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Meanwell, Nicholas A" sort="Meanwell, Nicholas A" uniqKey="Meanwell N" first="Nicholas A" last="Meanwell">Nicholas A. Meanwell</name><affiliation wicri:level="2"><nlm:affiliation>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author><author><name sortKey="Scola, Paul M" sort="Scola, Paul M" uniqKey="Scola P" first="Paul M" last="Scola">Paul M. Scola</name><affiliation wicri:level="2"><nlm:affiliation>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, United States.</nlm:affiliation><country xml:lang="fr">États-Unis</country><wicri:regionArea>Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492</wicri:regionArea><placeName><region type="state">Connecticut</region></placeName></affiliation></author></analytic><series><title level="j">Bioorganic & medicinal chemistry letters</title><idno type="eISSN">1464-3405</idno><imprint><date when="2017" type="published">2017</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Antiviral Agents (chemistry)</term><term>Antiviral Agents (pharmacokinetics)</term><term>Antiviral Agents (pharmacology)</term><term>Hepacivirus (drug effects)</term><term>Hepacivirus (physiology)</term><term>Humans</term><term>Membrane Fusion (drug effects)</term><term>Rats</term><term>Structure-Activity Relationship</term><term>Triazines (chemistry)</term><term>Triazines (pharmacokinetics)</term><term>Triazines (pharmacology)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Animaux</term><term>Antiviraux ()</term><term>Antiviraux (pharmacocinétique)</term><term>Antiviraux (pharmacologie)</term><term>Fusion membranaire ()</term><term>Hepacivirus ()</term><term>Hepacivirus (physiologie)</term><term>Humains</term><term>Rats</term><term>Relation structure-activité</term><term>Triazines ()</term><term>Triazines (pharmacocinétique)</term><term>Triazines (pharmacologie)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antiviral Agents</term><term>Triazines</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Antiviral Agents</term><term>Triazines</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term><term>Triazines</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Hepacivirus</term><term>Membrane Fusion</term></keywords><keywords scheme="MESH" qualifier="pharmacocinétique" xml:lang="fr"><term>Antiviraux</term><term>Triazines</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antiviraux</term><term>Triazines</term></keywords><keywords scheme="MESH" qualifier="physiologie" xml:lang="fr"><term>Hepacivirus</term></keywords><keywords scheme="MESH" qualifier="physiology" xml:lang="en"><term>Hepacivirus</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Humans</term><term>Rats</term><term>Structure-Activity Relationship</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Animaux</term><term>Antiviraux</term><term>Fusion membranaire</term><term>Hepacivirus</term><term>Humains</term><term>Rats</term><term>Relation structure-activité</term><term>Triazines</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">A series of potent and novel acylsulfonamide-bearing triazines were synthesized and the structure-activity relationships (SARs) as HCV entry inhibitors were evaluated. This acylsulfonamide series was derived from an early lead, 4-(4-(1-(4-chlorophenyl)cyclopropylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)benzoic acid wherein the carboxylic acid was replaced with an acylsulfonamide moiety. This structural modification provided a class of compounds which projected an additional vector off the terminus of the acylsulfonamide functionality as a means to drive activity. This effort led to the discovery of potent analogues within this series that demonstrated sub-nanomolar EC<sub>50</sub> values in the HCV pseudotype particle (HCVpp) assay.</div></front></TEI><affiliations><list><country><li>États-Unis</li></country><region><li>Connecticut</li></region></list><tree><country name="États-Unis"><region name="Connecticut"><name sortKey="Mull, Eric S" sort="Mull, Eric S" uniqKey="Mull E" first="Eric S" last="Mull">Eric S. Mull</name></region><name sortKey="Baldick, Carl J" sort="Baldick, Carl J" uniqKey="Baldick C" first="Carl J" last="Baldick">Carl J. Baldick</name><name sortKey="Cockett, Mark I" sort="Cockett, Mark I" uniqKey="Cockett M" first="Mark I" last="Cockett">Mark I. Cockett</name><name sortKey="Eggers, Betsy" sort="Eggers, Betsy" uniqKey="Eggers B" first="Betsy" last="Eggers">Betsy Eggers</name><name sortKey="Fang, Hua" sort="Fang, Hua" uniqKey="Fang H" first="Hua" last="Fang">Hua Fang</name><name sortKey="Jenkins, Susan" sort="Jenkins, Susan" uniqKey="Jenkins S" first="Susan" last="Jenkins">Susan Jenkins</name><name sortKey="Kramer, Melissa" sort="Kramer, Melissa" uniqKey="Kramer M" first="Melissa" last="Kramer">Melissa Kramer</name><name sortKey="Meanwell, Nicholas A" sort="Meanwell, Nicholas A" uniqKey="Meanwell N" first="Nicholas A" last="Meanwell">Nicholas A. Meanwell</name><name sortKey="Pokornowski, Kevin" sort="Pokornowski, Kevin" uniqKey="Pokornowski K" first="Kevin" last="Pokornowski">Kevin Pokornowski</name><name sortKey="Rajamani, Ramkumar" sort="Rajamani, Ramkumar" uniqKey="Rajamani R" first="Ramkumar" last="Rajamani">Ramkumar Rajamani</name><name sortKey="Scola, Paul M" sort="Scola, Paul M" uniqKey="Scola P" first="Paul M" last="Scola">Paul M. Scola</name><name sortKey="Sun, Li Qiang" sort="Sun, Li Qiang" uniqKey="Sun L" first="Li-Qiang" last="Sun">Li-Qiang Sun</name><name sortKey="Tenney, Daniel" sort="Tenney, Daniel" uniqKey="Tenney D" first="Daniel" last="Tenney">Daniel Tenney</name><name sortKey="Wang, Ying Kai" sort="Wang, Ying Kai" uniqKey="Wang Y" first="Ying-Kai" last="Wang">Ying-Kai Wang</name><name sortKey="Zhai, Guangzhi" sort="Zhai, Guangzhi" uniqKey="Zhai G" first="Guangzhi" last="Zhai">Guangzhi Zhai</name><name sortKey="Zhao, Qian" sort="Zhao, Qian" uniqKey="Zhao Q" first="Qian" last="Zhao">Qian Zhao</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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