Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase
Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-α production in mice and ex...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2005-05, Vol.15 (9), p.2409-2413 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Tamayo, Nuria Liao, Lillian Goldberg, Martin Powers, David Tudor, Yan-Yan Yu, Violeta Wong, Lu Min Henkle, Bradley Middleton, Scot Syed, Rashid Harvey, Timothy Jang, Graham Hungate, Randall Dominguez, Celia |
| description | Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-α production in mice and exhibited good efficacy in the rat collagen induced arthritis model.
Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-α production in mice and exhibited good efficacy in the rat collagen induced arthritis model. |
| doi_str_mv | 10.1016/j.bmcl.2005.02.010 |
| format | Article |
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Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-α production in mice and exhibited good efficacy in the rat collagen induced arthritis model.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2005.02.010</identifier><identifier>PMID: 15837335</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Binding Sites ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Drug Design ; Enzyme Inhibitors - chemical synthesis ; Enzyme Inhibitors - pharmacology ; Humans ; Indicators and Reagents ; Kinetics ; Medical sciences ; Microsomes, Liver - enzymology ; Models, Molecular ; Molecular Structure ; p38 Kinase inhibitors ; p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors ; p38 Mitogen-Activated Protein Kinases - chemistry ; Pharmacology. Drug treatments ; Protein Conformation ; Pyridazines ; Pyridazines - chemical synthesis ; Pyridazines - pharmacology ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (9), p.2409-2413</ispartof><rights>2005 Elsevier Ltd</rights><rights>2005 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c384t-6e68e08a5c81fcfd31b44980368bd4b7c4fa20c68731af81a5cf6167e74bf79f3</citedby><cites>FETCH-LOGICAL-c384t-6e68e08a5c81fcfd31b44980368bd4b7c4fa20c68731af81a5cf6167e74bf79f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2005.02.010$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,45974</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=16712689$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15837335$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Tamayo, Nuria</creatorcontrib><creatorcontrib>Liao, Lillian</creatorcontrib><creatorcontrib>Goldberg, Martin</creatorcontrib><creatorcontrib>Powers, David</creatorcontrib><creatorcontrib>Tudor, Yan-Yan</creatorcontrib><creatorcontrib>Yu, Violeta</creatorcontrib><creatorcontrib>Wong, Lu Min</creatorcontrib><creatorcontrib>Henkle, Bradley</creatorcontrib><creatorcontrib>Middleton, Scot</creatorcontrib><creatorcontrib>Syed, Rashid</creatorcontrib><creatorcontrib>Harvey, Timothy</creatorcontrib><creatorcontrib>Jang, Graham</creatorcontrib><creatorcontrib>Hungate, Randall</creatorcontrib><creatorcontrib>Dominguez, Celia</creatorcontrib><title>Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-α production in mice and exhibited good efficacy in the rat collagen induced arthritis model.
Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-α production in mice and exhibited good efficacy in the rat collagen induced arthritis model.</description><subject>Binding Sites</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Drug Design</subject><subject>Enzyme Inhibitors - chemical synthesis</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Humans</subject><subject>Indicators and Reagents</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>Microsomes, Liver - enzymology</subject><subject>Models, Molecular</subject><subject>Molecular Structure</subject><subject>p38 Kinase inhibitors</subject><subject>p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors</subject><subject>p38 Mitogen-Activated Protein Kinases - chemistry</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Conformation</subject><subject>Pyridazines</subject><subject>Pyridazines - chemical synthesis</subject><subject>Pyridazines - pharmacology</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMFK7DAUhoMoOld9ARfSje5aT5o0ScGNjHoVFF0ouAtpeqIZO-mYdIS5T387zIA7V4fD-f6fw0fICYWCAhUXs6KZ264oAaoCygIo7JAJ5YLnjEO1SyZQC8hVzd8OyJ-UZgCUA-f75IBWiknGqgm5vcbk30NmQpulVRg-xjVlvcsW_YBhyBar6FvzzwfMfPjwjR_6uLkzlT1ePWefPpiER2TPmS7h8XYektfbm5fpXf7w9Pd-evWQW6b4kAsUCkGZyirqrGsZbTivFTChmpY30nJnSrBCSUaNU3QEnaBCouSNk7Vjh-R807uI_dcS06DnPlnsOhOwXyYtpKzKsmYjWG5AG_uUIjq9iH5u4kpT0Gt7eqbX9vTanoZSj_bG0Om2fdnMsf2JbHWNwNkWMMmazkUTrE8_nJC0FKoeucsNh6OLb49RJ-sxWGx9RDvotve__fEfOBWM2g</recordid><startdate>20050502</startdate><enddate>20050502</enddate><creator>Tamayo, Nuria</creator><creator>Liao, Lillian</creator><creator>Goldberg, Martin</creator><creator>Powers, David</creator><creator>Tudor, Yan-Yan</creator><creator>Yu, Violeta</creator><creator>Wong, Lu Min</creator><creator>Henkle, Bradley</creator><creator>Middleton, Scot</creator><creator>Syed, Rashid</creator><creator>Harvey, Timothy</creator><creator>Jang, Graham</creator><creator>Hungate, Randall</creator><creator>Dominguez, Celia</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20050502</creationdate><title>Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase</title><author>Tamayo, Nuria ; Liao, Lillian ; Goldberg, Martin ; Powers, David ; Tudor, Yan-Yan ; Yu, Violeta ; Wong, Lu Min ; Henkle, Bradley ; Middleton, Scot ; Syed, Rashid ; Harvey, Timothy ; Jang, Graham ; Hungate, Randall ; Dominguez, Celia</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c384t-6e68e08a5c81fcfd31b44980368bd4b7c4fa20c68731af81a5cf6167e74bf79f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Binding Sites</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Drug Design</topic><topic>Enzyme Inhibitors - chemical synthesis</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>Humans</topic><topic>Indicators and Reagents</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>Microsomes, Liver - enzymology</topic><topic>Models, Molecular</topic><topic>Molecular Structure</topic><topic>p38 Kinase inhibitors</topic><topic>p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors</topic><topic>p38 Mitogen-Activated Protein Kinases - chemistry</topic><topic>Pharmacology. 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They demonstrated potent inhibition of LPS-induced TNF-α production in mice and exhibited good efficacy in the rat collagen induced arthritis model.
Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition of LPS-induced TNF-α production in mice and exhibited good efficacy in the rat collagen induced arthritis model.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>15837335</pmid><doi>10.1016/j.bmcl.2005.02.010</doi><tpages>5</tpages></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2005-05, Vol.15 (9), p.2409-2413 |
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| subjects | Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Humans Indicators and Reagents Kinetics Medical sciences Microsomes, Liver - enzymology Models, Molecular Molecular Structure p38 Kinase inhibitors p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors p38 Mitogen-Activated Protein Kinases - chemistry Pharmacology. Drug treatments Protein Conformation Pyridazines Pyridazines - chemical synthesis Pyridazines - pharmacology Structure-Activity Relationship |
| title | Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase |
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